BMS 182874
new
featured

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

Hodoodo CAT#: H584229

CAS#: 153042-42-3

Description: BMS 182874 is an endothelin receptor antagonist and antihypertensive agent.

Chemical Structure

img
BMS 182874
CAS# 153042-42-3
Instruction

Theoretical Analysis

Hodoodo Cat#: H584229
Name: BMS 182874
CAS#: 153042-42-3
Chemical Formula: C17H19N3O3S
Exact Mass: 345.11
Molecular Weight: 345.417
Elemental Analysis: C, 59.11; H, 5.54; N, 12.17; O, 13.90; S, 9.28

Price and Availability

Size Price Availability Quantity
50mg USD 450 2 Weeks
100mg USD 750 2 Weeks
200mg USD 1350 2 Weeks
500mg USD 2850 2 Weeks
1g USD 4450 2 Weeks
2g USD 6650 2 Weeks
Bulk inquiry

Related CAS #: 153042-42-3    

Synonym: BMS 182874; BMS-182874; BMS182874

IUPAC/Chemical Name: 1-Naphthalenesulfonamide, 5-(dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-

InChi Key: MJRGSRRZKSJHOE-UHFFFAOYSA-N

InChi Code: InChI=1S/C17H19N3O3S/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

SMILES Code: O=S(C1=C2C=CC=C(N(C)C)C2=CC=C1)(NC3=C(C)C(C)=NO3)=O

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

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:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 345.42 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.

Recalculate based on batch purity %
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
Formulation protocol:
In vitro protocol:
In vivo protocol:

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

1: Stein PD, Hunt JT, Floyd DM, Moreland S, Dickinson KE, Mitchell C, Liu EC, Webb ML, Murugesan N, Dickey J, et al. The discovery of sulfonamide endothelin antagonists and the development of the orally active ETA antagonist 5-(dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulf onamide. J Med Chem. 1994 Feb 4;37(3):329-31. PubMed PMID: 8308857.

2: Piovezan AP, D'Orléans-Juste P, Tonussi CR, Rae GA. Effects of endothelin-1 on capsaicin-induced nociception in mice. Eur J Pharmacol. 1998 Jun 12;351(1):15-22. PubMed PMID: 9698200.

3: Park JB, Schiffrin EL. Cardiac and vascular fibrosis and hypertrophy in aldosterone-infused rats: role of endothelin-1. Am J Hypertens. 2002 Feb;15(2 Pt 1):164-9. PubMed PMID: 11863252.

4: Scherer EQ, Herzog M, Wangemann P. Endothelin-1-induced vasospasms of spiral modiolar artery are mediated by rho-kinase-induced Ca(2+) sensitization of contractile apparatus and reversed by calcitonin gene-related Peptide. Stroke. 2002 Dec;33(12):2965-71. PubMed PMID: 12468798.

5: 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.

6: Holm P, Liska J, Franco-Cereceda A. The ETA receptor antagonist, BMS-182874, reduces acute hypoxic pulmonary hypertension in pigs in vivo. Cardiovasc Res. 1998 Mar;37(3):765-71. PubMed PMID: 9659461.

7: 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.

8: Seccia TM, Belloni AS, Kreutz R, Paul M, Nussdorfer GG, Pessina AC, Rossi GP. Cardiac fibrosis occurs early and involves endothelin and AT-1 receptors in hypertension due to endogenous angiotensin II. J Am Coll Cardiol. 2003 Feb 19;41(4):666-73. PubMed PMID: 12598081.

9: Bradbury RH, Bath C, Butlin RJ, Dennis M, Heys C, Hunt SJ, James R, Mortlock AA, Sumner NF, Tang EK, Telford B, Whiting E, Wilson C. New non-peptide endothelin-A receptor antagonists: synthesis, biological properties, and structure-activity relationships of 5-(dimethylamino)-N-pyridyl-,-N-pyrimidinyl-,-N-pyridazinyl-, and -N-pyrazinyl-1-naphthalenesulfonamides. J Med Chem. 1997 Mar 14;40(6):996-1004. PubMed PMID: 9083490.

10: Puppala BL, Matwyshyn G, Bhalla S, Gulati A. Evidence that morphine tolerance may be regulated by endothelin in the neonatal rat. Biol Neonate. 2004;86(2):138-44. Epub 2004 Jun 22. PubMed PMID: 15218283.

11: Khan H, Naylor RJ, Tuladhar BR. Pharmacological characterization of endothelin receptors-mediated contraction in the mouse isolated proximal and distal colon. Br J Pharmacol. 2006 Mar;147(6):607-11. PubMed PMID: 16432510; PubMed Central PMCID: PMC1751337.

12: 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.

13: Tostes RC, Touyz RM, He G, Chen X, Schiffrin EL. Contribution of endothelin-1 to renal activator protein-1 activation and macrophage infiltration in aldosterone-induced hypertension. Clin Sci (Lond). 2002 Aug;103 Suppl 48:25S-30S. PubMed PMID: 12193048.

14: Rossi GP, Cavallin M, Belloni AS, Mazzocchi G, Nussdorfer GG, Pessina AC, Sartore S. Aortic smooth muscle cell phenotypic modulation and fibrillar collagen deposition in angiotensin II-dependent hypertension. Cardiovasc Res. 2002 Jul;55(1):178-89. PubMed PMID: 12062721.

15: Kumar A, Morrison S, Gulati A. Effect of ETA receptor antagonists on cardiovascular responses induced by centrally administered sarafotoxin 6b: role of sympathetic nervous system. Peptides. 1997;18(6):855-64. PubMed PMID: 9285935.

16: Solini A, Santini E, Madec S, Cuccato S, Ferrannini E. Effects of endothelin-1 on fibroblasts from type 2 diabetic patients: Possible role in wound healing and tissue repair. Growth Factors. 2007 Dec;25(6):392-9. doi: 10.1080/08977190801892341. PubMed PMID: 18365870.

17: Webb ML, Bird JE, Liu EC, Rose PM, Serafino R, Stein PD, Moreland S. BMS-182874 is a selective, nonpeptide endothelin ETA receptor antagonist. J Pharmacol Exp Ther. 1995 Mar;272(3):1124-34. PubMed PMID: 7891325.

18: Ajayi AA, Newaz M, Hercule H, Saleh M, Bode CO, Oyekan AO. Endothelin-like action of Pausinystalia yohimbe aqueous extract on vascular and renal regional hemodynamics in Sprague Dawley rats. Methods Find Exp Clin Pharmacol. 2003 Dec;25(10):817-22. PubMed PMID: 14735230.

19: Modesti PA, Vanni S, Paniccia R, Bandinelli B, Bertolozzi I, Polidori G, Sani G, Neri Serneri GG. Characterization of endothelin-1 receptor subtypes in isolated human cardiomyocytes. J Cardiovasc Pharmacol. 1999 Sep;34(3):333-9. PubMed PMID: 10470989.

20: Hercule HC, Oyekan AO. Role of NO and cytochrome P-450-derived eicosanoids in ET-1-induced changes in intrarenal hemodynamics in rats. Am J Physiol Regul Integr Comp Physiol. 2000 Dec;279(6):R2132-41. PubMed PMID: 11080078.