BMS 182874 Hydrochloride | CAS#1215703-04-0 | Endothelin ETAR Antagonist

MedKoo Cat#: 524426 | Name: BMS 182874 Hydrochloride

Description:

WARNING: This product is for research use only, not for human or veterinary use.

BMS 182874 hydrochloride is a potent, selective, and competitive non-peptide endothelin ETAR antagonist. It displays > 1000-fold selectivity over ETB receptors. BMS 182874 hydrochloride inhibits ET-1-induced pressor response in vivo. It inhibits ET-1-induced pressor response, and also inhibits ET-1-induced longitudinal muscle contraction in vitro.

Chemical Structure

BMS 182874 Hydrochloride

CAS#1215703-04-0 (HCl)

Theoretical Analysis

MedKoo Cat#: 524426

Name: BMS 182874 Hydrochloride

CAS#: 1215703-04-0 (HCl)

Chemical Formula: C17H20ClN3O3S

Exact Mass: 0.0000

Molecular Weight: 381.88

Elemental Analysis: C, 53.47; H, 5.28; Cl, 9.28; N, 11.00; O, 12.57; S, 8.40

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Related CAS #

153042-42-3 (free base) 1215703-04-0 (HCl)

Synonym

BMS 182874; BMS-182874; BMS182874; BMS 182874 HCl; BMS 182874 hydrochloride

IUPAC/Chemical Name

5-(dimethylamino)-N-(3,4-dimethylisoxazol-5-yl)naphthalene-1-sulfonamide hydrochloride

InChi Key

UZZFRNZGYDOBAO-UHFFFAOYSA-N

InChi Code

InChI=1S/C17H19N3O3S.ClH/c1-11-12(2)18-23-17(11)19-24(21,22)16-10-6-7-13-14(16)8-5-9-15(13)20(3)4;/h5-10,19H,1-4H3;1H

SMILES Code

CC1=C(NS(=O)(C2=CC=CC3=C2C=CC=C3N(C)C)=O)ON=C1C.Cl

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO, not in water

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 381.88 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

1: Katyal T, Garg A, Budhiraja RD. Combination of daidzein, hemin and bms182874 halts the progression of diabetes-induced experimental nephropathy. Endocr Metab Immune Disord Drug Targets. 2013 Jun;13(2):152-62. PubMed PMID: 23701217. 2: Bhalla S, Ali I, Lee H, Andurkar SV, Gulati A. Potentiation of oxycodone antinociception in mice by agmatine and BMS182874 via an imidazoline I2 receptor-mediated mechanism. Pharmacol Biochem Behav. 2013 Jan;103(3):550-60. doi: 10.1016/j.pbb.2012.10.007. Epub 2012 Oct 26. PubMed PMID: 23103903. 3: Bhalla S, Andurkar SV, Gulati A. Involvement of α₂-adrenoceptors, imidazoline, and endothelin-A receptors in the effect of agmatine on morphine and oxycodone-induced hypothermia in mice. Fundam Clin Pharmacol. 2013 Oct;27(5):498-509. doi: 10.1111/j.1472-8206.2012.01046.x. Epub 2012 Jun 11. PubMed PMID: 22681550. 4: Andurkar SV, Gendler L, Gulati A. Tramadol antinociception is potentiated by clonidine through α₂-adrenergic and I₂-imidazoline but not by endothelin ET(A) receptors in mice. Eur J Pharmacol. 2012 May 15;683(1-3):109-15. doi: 10.1016/j.ejphar.2012.03.016. Epub 2012 Mar 16. PubMed PMID: 22449379. 5: Arteaga JL, Orensanz LM, Martínez MP, Barahona MV, Recio P, Martínez-Sáenz A, Fernandes VS, Ribeiro AS, García-Sacristán A, Prieto D, Hernández M. Mechanisms involved in endothelin-1-induced contraction of the pig urinary bladder neck. Neurourol Urodyn. 2012 Jan;31(1):156-61. doi: 10.1002/nau.21187. Epub 2011 Sep 26. PubMed PMID: 21953705. 6: Bhalla S, Andurkar SV, Gulati A. Study of adrenergic, imidazoline, and endothelin receptors in clonidine-, morphine-, and oxycodone-induced changes in rat body temperature. Pharmacology. 2011;87(3-4):169-79. doi: 10.1159/000324537. Epub 2011 Mar 8. PubMed PMID: 21389745. 7: Briyal S, Philip T, Gulati A. Endothelin-A receptor antagonists prevent amyloid-β-induced increase in ETA receptor expression, oxidative stress, and cognitive impairment. J Alzheimers Dis. 2011;23(3):491-503. doi: 10.3233/JAD-2010-101245. PubMed PMID: 21116051. 8: Bhalla S, Rapolaviciute V, Gulati A. Determination of α(2)-adrenoceptor and imidazoline receptor involvement in augmentation of morphine and oxycodone analgesia by agmatine and BMS182874. Eur J Pharmacol. 2011 Jan 25;651(1-3):109-21. doi: 10.1016/j.ejphar.2010.10.090. Epub 2010 Nov 27. PubMed PMID: 21114998. 9: Bhalla S, Zhang Z, Patterson N, Gulati A. Effect of endothelin-A receptor antagonist on mu, delta and kappa opioid receptor-mediated antinociception in mice. Eur J Pharmacol. 2010 Jun 10;635(1-3):62-71. doi: 10.1016/j.ejphar.2010.03.003. Epub 2010 Mar 19. PubMed PMID: 20303944. 10: Gulati A, Bhalla S, Matwyshyn G, Zhang Z, Andurkar SV. Determination of adrenergic and imidazoline receptor involvement in augmentation of morphine and oxycodone analgesia by clonidine and BMS182874. Pharmacology. 2009;83(1):45-58. doi: 10.1159/000178812. Epub 2008 Dec 4. PubMed PMID: 19052482. 11: Chavanpatil MD, Rajeshkumar NV, Gulati A. Determination of endothelin antagonist BMS182874 in plasma by high-performance liquid chromatography. Pharmazie. 2006 Jun;61(6):525-7. PubMed PMID: 16826972. 12: Matwyshyn GA, Bhalla S, Gulati A. Endothelin ETA receptor blockade potentiates morphine analgesia but does not affect gastrointestinal transit in mice. Eur J Pharmacol. 2006 Aug 14;543(1-3):48-53. Epub 2006 May 26. PubMed PMID: 16814278. 13: Puppala BL, Bhalla S, Matwyshyn G, Gulati A. Involvement of central endothelin receptors in neonatal morphine withdrawal. Exp Biol Med (Maywood). 2006 Jun;231(6):1157-60. PubMed PMID: 16741068. 14: Bhalla S, Ciaccio N, Wang ZJ, Gulati A. Involvement of endothelin in morphine tolerance in neuroblastoma (SH-SY5Y) cells. Exp Biol Med (Maywood). 2006 Jun;231(6):1152-6. PubMed PMID: 16741067. 15: Puppala BL, Bhalla S, Matwyshyn G, Gulati A. Role of endothelin (ETA) receptors in neonatal morphine withdrawal. Peptides. 2006 Jun;27(6):1514-9. Epub 2005 Nov 15. PubMed PMID: 16293342. 16: Bhalla S, Matwyshyn G, Gulati A. Morphine tolerance does not develop in mice treated with endothelin-A receptor antagonists. Brain Res. 2005 Dec 7;1064(1-2):126-35. Epub 2005 Nov 14. PubMed PMID: 16289404. 17: Callera GE, Tostes RC, Yogi A, Montezano AC, Touyz RM. Endothelin-1-induced oxidative stress in DOCA-salt hypertension involves NADPH-oxidase-independent mechanisms. Clin Sci (Lond). 2006 Feb;110(2):243-53. PubMed PMID: 16271043. 18: Montezano AC, Callera GE, Mota AL, Fortes ZB, Nigro D, Carvalho MH, Zorn TM, Tostes RC. Endothelin-1 contributes to the sexual differences in renal damage in DOCA-salt rats. Peptides. 2005 Aug;26(8):1454-62. Epub 2005 Apr 19. PubMed PMID: 16042985. 19: Gulati A, Bhalla S, Matwyshyn G. A novel combination of opiates and endothelin antagonists to manage pain without any tolerance development. J Cardiovasc Pharmacol. 2004 Nov;44 Suppl 1:S129-31. PubMed PMID: 15838261. 20: Xavier FE, Yogi A, Callera GE, Tostes RC, Alvarez Y, Salaices M, Alonso MJ, Rossoni LV. Contribution of the endothelin and renin-angiotensin systems to the vascular changes in rats chronically treated with ouabain. Br J Pharmacol. 2004 Nov;143(6):794-802. Epub 2004 Oct 11. PubMed PMID: 15477225; PubMed Central PMCID: PMC1575934.