SB-209670 | CAS#157659-79-5 | endothelin receptor antagonist

MedKoo Cat#: 526690 | Name: SB-209670

Description:

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

SB-209670 is a endothelin receptor antagonist. SB 209670 inhibits the arrhythmogenic actions of endothelin-1 in the anesthetized dog. SB 209670 selectively antagonize vascular endothelial versus vascular smooth muscle ET(B)-receptor activity in the rat. (last updated: 6/18/2016).

Chemical Structure

SB-209670

CAS#157659-79-5

Theoretical Analysis

MedKoo Cat#: 526690

Name: SB-209670

CAS#: 157659-79-5

Chemical Formula: C29H28O9

Exact Mass: 520.1733

Molecular Weight: 520.53

Elemental Analysis: C, 66.92; H, 5.42; O, 27.66

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.

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Related CAS #

No Data

Synonym

SB-209670; SB 209670; SB209670.

IUPAC/Chemical Name

(1S,2R,3S)-1-(1,3-benzodioxol-5-yl)-3-[2-(carboxymethoxy)-4-methoxyphenyl]-5-propoxy-2,3-dihydro-1H-indene-2-carboxylic acid

InChi Key

UUAVCCWBNUITBB-UPRLRBBYSA-N

InChi Code

InChI=1S/C29H28O9/c1-3-10-35-18-6-7-19-21(12-18)27(20-8-5-17(34-2)13-23(20)36-14-25(30)31)28(29(32)33)26(19)16-4-9-22-24(11-16)38-15-37-22/h4-9,11-13,26-28H,3,10,14-15H2,1-2H3,(H,30,31)(H,32,33)/t26-,27+,28+/m0/s1

SMILES Code

O=C([C@@H]1[C@@H](C2=CC=C(OCO3)C3=C2)C4=C(C=C(OCCC)C=C4)[C@H]1C5=CC=C(C=C5OCC(O)=O)OC)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, 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 520.53 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: Burrell KM, Molenaar P, Dawson PJ, Kaumann AJ. Contractile and arrhythmic effects of endothelin receptor agonists in human heart in vitro: blockade with SB 209670. J Pharmacol Exp Ther. 2000 Jan;292(1):449-59. PubMed PMID: 10604982. 2: Bunting MW, Widdop RE. Differential haemodynamic effects of endothelin receptor antagonist, SB 209670, in conscious hypertensive and normotensive rats. Eur J Pharmacol. 1999 Sep 17;381(1):13-21. PubMed PMID: 10528129. 3: Freed MI, Wilson DE, Thompson KA, Harris RZ, Ilson BE, Jorkasky DK. Pharmacokinetics and pharmacodynamics of SB 209670, an endothelin receptor antagonist: effects on the regulation of renal vascular tone. Clin Pharmacol Ther. 1999 May;65(5):473-82. PubMed PMID: 10340912. 4: Schroeder RL, Keiser JA, Cheng XM, Haleen SJ. PD 142893, SB 209670, and BQ 788 selectively antagonize vascular endothelial versus vascular smooth muscle ET(B)-receptor activity in the rat. J Cardiovasc Pharmacol. 1998 Dec;32(6):935-43. PubMed PMID: 9869499. 5: Douglas SA, Nichols AJ, Feuerstein GZ, Elliott JD, Ohlstein EH. SB 209670 inhibits the arrhythmogenic actions of endothelin-1 in the anesthetized dog. J Cardiovasc Pharmacol. 1998;31 Suppl 1:S99-102. PubMed PMID: 9595411. 6: Ishikawa A, Suzuki K, Fujita K. Effect of the endothelin receptor antagonist, SB 209670 on cyclosporine-induced nephrotoxicity. Transplant Proc. 1998 Feb;30(1):40-2. PubMed PMID: 9474951. 7: Hay DW, Luttmann MA. Nonpeptide endothelin receptor antagonists. IX. Characterization of endothelin receptors in guinea pig bronchus with SB 209670 and other endothelin receptor antagonists. J Pharmacol Exp Ther. 1997 Feb;280(2):959-65. PubMed PMID: 9023312. 8: Gardiner SM, Kemp PA, March JE, Bennett T. Influence of aminoguanidine and the endothelin antagonist, SB 209670, on the regional haemodynamic effects of endotoxaemia in conscious rats. Br J Pharmacol. 1996 Aug;118(7):1822-8. PubMed PMID: 8842449; PubMed Central PMCID: PMC1909836. 9: Nambi P, Pullen M, Wu HL, Lee D, Saunders D, Heys R, Aiyar N, Leber J, Elliott J, Brooks D, Ohlstein E, Ruffolo R. Nonpeptide endothelin receptor antagonists. VII: Binding characteristics of [3H]SB 209670, a novel nonpeptide antagonist of endothelin receptors. J Pharmacol Exp Ther. 1996 Jun;277(3):1567-71. PubMed PMID: 8667224. 10: Ruetten H, Thiemermann C, Vane JR. Effects of the endothelin receptor antagonist, SB 209670, on circulatory failure and organ injury in endotoxic shock in the anaesthetized rat. Br J Pharmacol. 1996 May;118(1):198-204. PubMed PMID: 8733596; PubMed Central PMCID: PMC1909477. 11: Gardiner SM, Kemp PA, March JE, Bennett T. Effects of dexamethasone and SB 209670 on the regional haemodynamic responses to lipopolysaccharide in conscious rats. Br J Pharmacol. 1996 May;118(1):141-9. PubMed PMID: 8733587; PubMed Central PMCID: PMC1909479. 12: Brooks DP, DePalma PD. Blockade of radiocontrast-induced nephrotoxicity by the endothelin receptor antagonist, SB 209670. Nephron. 1996;72(4):629-36. PubMed PMID: 8730433. 13: Brooks DP, Contino LC. Prevention of cyclosporine A-induced renal vasoconstriction by the endothelin receptor antagonist SB 209670. Eur J Pharmacol. 1995 Dec 29;294(2-3):571-6. PubMed PMID: 8750720. 14: Gardiner SM, March JE, Kemp PA, Mullins JJ, Bennett T. Haemodynamic effects of losartan and the endothelin antagonist, SB 209670, in conscious, transgenic ((mRen-2)27), hypertensive rats. Br J Pharmacol. 1995 Oct;116(4):2237-44. PubMed PMID: 8564254; PubMed Central PMCID: PMC1908969. 15: Gellai M, Jugus M, Fletcher T, Nambi P, Ohlstein EH, Elliott JD, Brooks DP. Nonpeptide endothelin receptor antagonists. V: Prevention and reversal of acute renal failure in the rat by SB 209670. J Pharmacol Exp Ther. 1995 Oct;275(1):200-6. PubMed PMID: 7562550. 16: Gardiner SM, Kemp PA, March JE, Bennett T. Enhancement of the hypotensive and vasodilator effects of endotoxaemia in conscious rats by the endothelin antagonist, SB 209670. Br J Pharmacol. 1995 Sep;116(2):1718-9. PubMed PMID: 8528549; PubMed Central PMCID: PMC1909072. 17: Douglas SA, Gellai M, Ezekiel M, Feuerstein GZ, Elliott JD, Ohlstein EH. Antihypertensive actions of the novel nonpeptide endothelin receptor antagonist SB 209670. Hypertension. 1995 Apr;25(4 Pt 2):818-22. PubMed PMID: 7721437. 18: Klemm P, Warner TD, Willis D, Moore AR, Vane JR. Coronary vasoconstriction in vitro in the hearts of polyarthritic rats: effectiveness of in vivo treatment with the endothelin receptor antagonist SB 209670. Br J Pharmacol. 1995 Apr;114(7):1327-8. PubMed PMID: 7606336; PubMed Central PMCID: PMC1510275. 19: Wellings RP, Corder R, Vane JR. Lack of effect of ET antibody or SB 209670 on endotoxin-induced renal failure. J Cardiovasc Pharmacol. 1995;26 Suppl 3:S476-8. PubMed PMID: 8587451. 20: Douglas SA, Vickery-Clark LM, Louden C, Elliott JD, Ohlstein EH. Endothelin receptor subtypes in the pathogenesis of angioplasty-induced neointima formation in the rat: a comparison of selective ETA receptor antagonism and dual ETA/ETB receptor antagonism using BQ-123 and SB 209670. J Cardiovasc Pharmacol. 1995;26 Suppl 3:S186-9. PubMed PMID: 8587358.