CRFR-Agonists-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/CRFR.html CRFRCorticotropin-releasing Factor ReceptorThe CRFR (Corticotropin-releasing Factor Receptor, CRHR) belongs to the G-coupled receptor superfamily. Two receptor subtypes, CRF receptor and CRF receptor, and several splice variants for both receptor subt

2、ypes have been discovered. CRF itself has a1 2greater affinity for CRF receptors while urocortin 1 (Ucn 1) binds with high affinity to both receptors and Ucn 2 and Ucn 3 both1preferentially bind to CRF receptors.2Two CRF receptor subtypes are encoded by distinct genes which exhibit diverse alternati

3、ve pre-mRNA splicing patterns resulting in multiple variants derived from partial or total exon deletions or insertions. With regard to the nine human CRF variants, CRF ,1 1a-idescribed, CRF a being the main wild type functional receptor while the other isoforms may modulate CRF signaling. For the C

4、RF ,1 2three functionally active splice variants, CRF , have been described in humans.2a-cwww.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/CRFR.html CRFR HYPERLINK https:/www.MedChemE/Targets/CRFR.html HYPERLINK https:/www.MedChemE/Targets/CRFR.html Inhibitors, HYPERLINK https:/www.MedChemE/Targ

5、ets/CRFR.html HYPERLINK https:/www.MedChemE/Targets/CRFR.html Agonists, HYPERLINK https:/www.MedChemE/Targets/CRFR.html HYPERLINK https:/www.MedChemE/Targets/CRFR.html Antagonists, HYPERLINK https:/www.MedChemE/Targets/CRFR.html HYPERLINK https:/www.MedChemE/Targets/CRFR.html Activators HYPERLINK ht

6、tps:/www.MedChemE/Targets/CRFR.html HYPERLINK https:/www.MedChemE/Targets/CRFR.html & HYPERLINK https:/www.MedChemE/Targets/CRFR.html HYPERLINK https:/www.MedChemE/Targets/CRFR.html Modulators HYPERLINK https:/www.MedChemE/antisauvagine-30.html Antisauvagine-30(aSvg-30) Cat. No.: HY-P1107 HYPERLINK

7、https:/www.MedChemE/antisauvagine-30-tfa.html Antisauvagine-30 HYPERLINK https:/www.MedChemE/antisauvagine-30-tfa.html HYPERLINK https:/www.MedChemE/antisauvagine-30-tfa.html TFA(aSvg-30 TFA) Cat. No.: HY-P1107AAntisauvagine-30 (aSvg-30) is a potent,competitive and selective CRF receptor2antagonist

8、with K values of 1.4 nM and 153.6 nMdfor mouse CRF and rat2CRF receptors, respectively.1Antisauvagine-30 TFA (aSvg-30 TFA) is a potent,highly selective and competitive CRF receptor2peptidic antagonist. Antisauvagine-30 TFA exhibitsa K of 1.4 nM and 150 nM for mCRFR2 and CRFR1,drespectively.Purity: 9

9、8%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.01%Clinical Data: No Development ReportedSize: 5 mg, 10 mg HYPERLINK https:/www.MedChemE/cortagine.html CortagineCat. No.: HY-P2287 HYPERLINK https:/www.MedChemE/Corticotropin-releasing-factor-human.html Corticotropin-releasing HYPER

10、LINK https:/www.MedChemE/Corticotropin-releasing-factor-human.html HYPERLINK https:/www.MedChemE/Corticotropin-releasing-factor-human.html factor HYPERLINK https:/www.MedChemE/Corticotropin-releasing-factor-human.html HYPERLINK https:/www.MedChemE/Corticotropin-releasing-factor-human.html (human)(Hu

11、man CRF; Human corticotropin-releasing factor) Cat. No.: HY-P0086Cortagine is a specific corticotropin-releasingfactor receptor subtype 1 (CRF1) agonist with anIC of 2.6 nM for rCRF1. Cortagine is an50anxiolytic and antidepressive drug in the mousemodel.Corticotropin-releasing factor human (Human CR

12、F)stimulates the synthesis and secretion ofadrenocorticotropin in the anterior pituitary.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mgPurity: 98.44%Clinical Data: No Development ReportedSize: 250 g, 500 g, 1 mg, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/corticotropin-relea

13、sing-factor-human-acetate.html Corticotropin-releasing HYPERLINK https:/www.MedChemE/corticotropin-releasing-factor-human-acetate.html HYPERLINK https:/www.MedChemE/corticotropin-releasing-factor-human-acetate.html factor HYPERLINK https:/www.MedChemE/corticotropin-releasing-factor-human-acetate.htm

14、l HYPERLINK https:/www.MedChemE/corticotropin-releasing-factor-human-acetate.html (human) HYPERLINK https:/www.MedChemE/corticotropin-releasing-factor-human-acetate.html HYPERLINK https:/www.MedChemE/corticotropin-releasing-factor-human-acetate.html (acetate) HYPERLINK https:/www.MedChemE/corticotro

15、pin-releasing-factor-human-acetate.html (Human CRFacetate; Human corticotropin-releasing factor acetate) Cat. No.: HY-P0086A HYPERLINK https:/www.MedChemE/CP_316311.html CP HYPERLINK https:/www.MedChemE/CP_316311.html HYPERLINK https:/www.MedChemE/CP_316311.html 316311Cat. No.: HY-14129Corticotropin

16、-releasing factor human acetate(Human CRF acetate) stimulates the synthesis andsecretion of adrenocorticotropin in the anteriorpituitary.CP 316311 is a potent and selective CRF1receptor antagonist with an IC value of 6.8 nM.50Purity: 98.25%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity

17、: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/CP_376395.html CP HYPERLINK https:/www.MedChemE/CP_376395.html HYPERLINK https:/www.MedChemE/CP_376395.html 376395 HYPERLINK https:/www.MedChemE/CP_376395.html HYPERLINK https:/www.MedChemE/crf-6-33-human.html

18、CRF(6-33)(human)Cat. No.: HY-14130 Cat. No.: HY-P1297CP 376395 is a potent and selective Corticotropinreleasing factor 1 (CRF1) receptor antagonist.CRF(6-33)(human) is a CRF binding protein(CRF-BP) ligand inhibitor. CRF(6-33)(human)competitively binds the CRF-BP but not thepost-synaptic CRF receptor

19、s. CRF(6-33)(human) hasanti-obesity effect.Purity: 99.71%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/crf-6-33-human-tfa.html CRF(6-33)(human) HYPERLINK https:/

20、www.MedChemE/crf-6-33-human-tfa.html HYPERLINK https:/www.MedChemE/crf-6-33-human-tfa.html TFA HYPERLINK https:/www.MedChemE/crf-6-33-human-tfa.html HYPERLINK https:/www.MedChemE/CRF,bovine.html CRF, HYPERLINK https:/www.MedChemE/CRF,bovine.html HYPERLINK https:/www.MedChemE/CRF,bovine.html bovineCa

21、t. No.: HY-P1297A(Corticotropin Releasing Factor bovine) Cat. No.: HY-P1533CRF(6-33)(human) TFA is a CRF binding protein(CRF-BP) ligand inhibitor. CRF(6-33)(human) TFAcompetitively binds the CRF-BP but not thepost-synaptic CRF receptors. CRF(6-33)(human) TFAhas anti-obesity effect.CRF, bovine is a p

22、otent agonist of CRF receptor,and displaces 125I-Tyrovine CRF with a K of 3.52inM.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE

23、/crf-bovine-tfa.html CRF, HYPERLINK https:/www.MedChemE/crf-bovine-tfa.html HYPERLINK https:/www.MedChemE/crf-bovine-tfa.html bovine HYPERLINK https:/www.MedChemE/crf-bovine-tfa.html HYPERLINK https:/www.MedChemE/crf-bovine-tfa.html TFA(Corticotropin Releasing Factor bovine TFA) Cat. No.: HY-P1533A

24、HYPERLINK https:/www.MedChemE/Emicerfont.html Emicerfont(GW876008) Cat. No.: HY-14367CRF, bovine (TFA) is a potent agonist of CRFreceptor, and displaces 125I-Tyrovine CRF with aK of 3.52 nM.iEmicerfont is a corticotropin-releasing factortype 1 (CRF ) receptor antagonist with an1 IC50of 66 nM.Purity:

25、 96.50%Clinical Data: No Development ReportedSize: 500 g, 1 mg, 5 mgPurity: 98%Clinical Data: Phase 2Size: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/k41498.html K41498 HYPERLINK https:/www.MedChemE/k41498.html HYPERLINK https:/www.MedChemE/nbi-27914.html NBI-27914Cat. No.: HY-P1106 Cat. No.: HY-13554

26、2K41498 is a potent and highly selectiveCRF2 receptor antagonist with K valuesiof 0.66 nM, 0.62 nM and 425 nM for human CRF ,2CRF and CRF receptors respectively.2 1NBI-27914 is a potent and selective antagonist ofCRFR1. The CRF receptors, CRFR1 and CRFR2, aremembers of the G protein-coupled receptor

27、superfamily.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/nbi-27914-hydrochloride.html NBI-27914 HYPERLINK https:/www.MedChemE/nbi-27914-hydrochloride.html HYPERLINK https:/www.MedChemE

28、/nbi-27914-hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/nbi-27914-hydrochloride.html HYPERLINK https:/www.MedChemE/nvs-crf38.html NVS-CRF38Cat. No.: HY-103376 Cat. No.: HY-12339NBI-27914 (hydrochloride) is a selectiveCorticotropin-Releasing Factor 1 (CRF1) receptorantagonist with a

29、 K value of 1.7 nM.iNVS-CRF38 is a novel corticotropin-releasingfactor receptor 1 (CRF1) antagonist with low watersolubility. IC50 value: Target: CRF1 antagonist.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLI

30、NK https:/www.MedChemE/Pexacerfont.html Pexacerfont HYPERLINK https:/www.MedChemE/Pexacerfont.html HYPERLINK https:/www.MedChemE/R121919.html R121919(BMS-562086) Cat. No.: HY-12127 (NBI30775) Cat. No.: HY-14127Pexacerfont is a selective corticotropin-releasingfactor (CRF ) receptor antagonist with o

31、f1 IC506.10.6 nM for human CRF receptor.1R121919 (NBI30775) is a potent small-moleculeCRF1 receptor antagonist with a K of 2 to 5 nMifor the CRF1 receptor and over 1000-fold weakeractivity at the CRF2 receptor, CRF-bindingprotein, or 70 other receptor types.Purity: 99.97%Clinical Data: Phase 3Size:

32、10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mgPurity: 99.84%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg HYPERLINK https:/www.MedChemE/sauvagine.html Sauvagine HYPERLINK https:/www.MedChemE/sauvagine.html HYPERLINK https:/www.MedChemE/sauvagine-tfa.html Sauvagine HY

33、PERLINK https:/www.MedChemE/sauvagine-tfa.html HYPERLINK https:/www.MedChemE/sauvagine-tfa.html TFACat. No.: HY-P1298 Cat. No.: HY-P1298ASauvagine, a 40-amino-acid neuropeptide from theskin of the frog, is a mammalian CRF agonist.Sauvagine is effective at releasing ACTH from ratpituitary cells. Sauv

34、agine possesses a number ofpharmacological actions on diuresis, thecardiovascular system and endocrine glands.Sauvagine TFA, a 40-amino-acid neuropeptide fromthe skin of the frog, is a mammalian CRFagonist. Sauvagine TFA is effective at releasingACTH from rat pituitary cells.Purity: 98%Clinical Data

35、: No Development ReportedSize: 1 mg, 5 mgPurity: 95.17%Clinical Data: No Development ReportedSize: 5 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/urocortin-ii-human.html Urocortin HYPERLINK https:/www.MedChemE/urocortin-ii-human.html HYPERLINK https:/www.MedChemE/urocortin-ii-human.html II, HYPERL

36、INK https:/www.MedChemE/urocortin-ii-human.html HYPERLINK https:/www.MedChemE/urocortin-ii-human.html human HYPERLINK https:/www.MedChemE/urocortin-ii-human.html HYPERLINK https:/www.MedChemE/urocortin-ii-human-tfa.html Urocortin HYPERLINK https:/www.MedChemE/urocortin-ii-human-tfa.html HYPERLINK ht

37、tps:/www.MedChemE/urocortin-ii-human-tfa.html II, HYPERLINK https:/www.MedChemE/urocortin-ii-human-tfa.html HYPERLINK https:/www.MedChemE/urocortin-ii-human-tfa.html human HYPERLINK https:/www.MedChemE/urocortin-ii-human-tfa.html HYPERLINK https:/www.MedChemE/urocortin-ii-human-tfa.html TFACat. No.:

38、 HY-P1752 Cat. No.: HY-P1752AUrocortin II (human) is a selective endogenouspeptide agonist of type-2 corticotropin-releasingfactor (CRF2) receptor. For investigating therole of the CRF (2) receptor in ingestivebehavior.Urocortin II, human (TFA) is a selectiveendogenous peptide agonist of type-2corti

39、cotropin-releasing factor (CRF2) receptor.For investigating the role of the CRF (2) receptorin ingestive behavior.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/urocortin-iii-mouse.html

40、Urocortin HYPERLINK https:/www.MedChemE/urocortin-iii-mouse.html HYPERLINK https:/www.MedChemE/urocortin-iii-mouse.html III, HYPERLINK https:/www.MedChemE/urocortin-iii-mouse.html HYPERLINK https:/www.MedChemE/urocortin-iii-mouse.html mouse HYPERLINK https:/www.MedChemE/urocortin-iii-mouse.html HYPE

41、RLINK https:/www.MedChemE/urocortin-iii-mouse-tfa.html Urocortin HYPERLINK https:/www.MedChemE/urocortin-iii-mouse-tfa.html HYPERLINK https:/www.MedChemE/urocortin-iii-mouse-tfa.html III, HYPERLINK https:/www.MedChemE/urocortin-iii-mouse-tfa.html HYPERLINK https:/www.MedChemE/urocortin-iii-mouse-tfa

42、.html mouse HYPERLINK https:/www.MedChemE/urocortin-iii-mouse-tfa.html HYPERLINK https:/www.MedChemE/urocortin-iii-mouse-tfa.html TFACat. No.: HY-P1858 Cat. No.: HY-P1858AUrocortin III, mouse is a corticotropin-releasingfactor (CRF)-related peptide. Urocortin IIIpreferentially binds and activates CR

43、F-R2.Urocortin III (Ucn3) is a known component of thebehavioral stress response system.Urocortin III, mouse TFA is acorticotropin-releasing factor (CRF)-relatedpeptide. Urocortin III preferentially binds andactivates CRF-R2. Urocortin III (Ucn3) is a knowncomponent of the behavioral stress responses

44、ystem.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.56%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/Urocortin,_human.html Urocortin, HYPERLINK https:/www.MedChemE/Urocortin,_human.html HYPERLINK https:/www.MedChemE/Urocorti

45、n,_human.html human HYPERLINK https:/www.MedChemE/Urocortin,_human.html (Urocortin (human); Human urocortin; Humanurocortin 1; Human urocortin I) Cat. No.: HY-P1295 HYPERLINK https:/www.MedChemE/Urocortin,_rat.html Urocortin, HYPERLINK https:/www.MedChemE/Urocortin,_rat.html HYPERLINK https:/www.Med

46、ChemE/Urocortin,_rat.html rat(Urocortin (Rattus norvegicus); Rat urocortin; ) Cat. No.: HY-P1296Urocortin, human, a 40-aa neuropeptide, acts as aselective agonist of endogenous CRF receptor,2with Ks of 0.4, 0.3, and 0.5 nM for hCRF ,i 1rCRF and mCRF , respectively.2 2Urocortin, rat (Urocortin (Rattu

47、s norvegicus) isa neuropeptide and a potent endogenous CRFRagonist with Ks of 13 nM, 1.5 nM, and 0.97 nM forihuman CRF1, rat CRF2 and mouseCRF , respectively.2Purity: 98.43%Clinical Data: No Development ReportedSize: 500 g, 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 500 g, 1 mg

48、, 5 mg HYPERLINK https:/www.MedChemE/urocortin-rat-tfa.html Urocortin, HYPERLINK https:/www.MedChemE/urocortin-rat-tfa.html HYPERLINK https:/www.MedChemE/urocortin-rat-tfa.html rat HYPERLINK https:/www.MedChemE/urocortin-rat-tfa.html HYPERLINK https:/www.MedChemE/urocortin-rat-tfa.html TFA HYPERLINK

49、 https:/www.MedChemE/urocortin-rat-tfa.html HYPERLINK https:/www.MedChemE/Urotensin_I.html Urotensin HYPERLINK https:/www.MedChemE/Urotensin_I.html HYPERLINK https:/www.MedChemE/Urotensin_I.html I(Urocortin (Rattus norvegicus) (TFA); Rat urocortin TFA) Cat. No.: HY-P1296A (Catostomus urotensin I) Ca

50、t. No.: HY-P1542Urocortin, rat TFA (Urocortin (Rattus norvegicus)TFA) is a neuropeptide and a potent endogenousCRFR agonist with Ks of 13 nM, 1.5 nM, and 0.97inM for human CRF1, rat CRF2 and mouseCRF , respectively.2Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgUrotensin I (Catost

51、omus urotensin I), a CRF-likeneuropeptide, acts as an agonist of CRF receptorwith pEC s of 11.46, 9.36 and 9.85 for human50CRF , human CRF and rat CRF receptors in CHO1 2 2cells, and Ks of 0.4, 1.8, and 5.7 nM for hCRF ,i 1rCRF and mCRF receptors, respectively.2 2Purity: 98%Clinical Data: No Develop

52、ment ReportedSize: 500 g, 1 mg, 5 mg HYPERLINK https:/www.MedChemE/urotensin-i-tfa.html Urotensin HYPERLINK https:/www.MedChemE/urotensin-i-tfa.html HYPERLINK https:/www.MedChemE/urotensin-i-tfa.html I HYPERLINK https:/www.MedChemE/urotensin-i-tfa.html HYPERLINK https:/www.MedChemE/urotensin-i-tfa.html TFA HYPERLINK https:/www.MedChemE/urotensin-i-tfa.html HYPERLINK https:/www.MedChemE/Verucerfont.html Veruce