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BMS 182874

Catalog No. T26841 CAS 153042-42-3

Synonyms: BMS182874, BMS-182874

BMS 182874 is an orally effective and highly selective endothelin receptor ETA antagonist with an IC50 value of 0.150 μM for ETA and a Ki value of 0.055 μM for ETA.BMS 182874 is able to reduce arterial pressure in a rat hypertension model induced by Deoxycorticosterone acetate. BMS 182874 was able to reduce Deoxycorticosterone-induced arterial pressure in a rat model of hypertension and can be used to study cardiovascular disease.

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BMS 182874, CAS 153042-42-3

Pack Size	Availability	Price/USD
1 mg	In stock	$ 85.00
5 mg	In stock	$ 200.00
10 mg	In stock	$ 330.00
25 mg	In stock	$ 557.00
50 mg	In stock	$ 783.00
100 mg	In stock	$ 1,090.00
500 mg	In stock	$ 2,230.00

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Purity: 98.38%

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Description	BMS 182874 is an orally effective and highly selective endothelin receptor ETA antagonist with an IC50 value of 0.150 μM for ETA and a Ki value of 0.055 μM for ETA.BMS 182874 is able to reduce arterial pressure in a rat hypertension model induced by Deoxycorticosterone acetate. BMS 182874 was able to reduce Deoxycorticosterone-induced arterial pressure in a rat model of hypertension and can be used to study cardiovascular disease.
Targets&IC50	ETA:0.150 μM, ETA:0.055 μM(Ki )
In vitro	BMS-182874 (dimethyla minonalogue 11) is an effective functional antagonist of ETA-induced intracellular Ca2+ increase, with an IC50 value of 0.150 μM in vs-A10 cells. Ki value is 0.055 μM. The KB value in the rabbit carotid artery ring is 0.520 μM/[1]
In vivo	BMS 182874 (100 μM/kg; Single oral) administration causes a slow decrease of 25% in arterial blood pressure from the control level. After 12 and 24 hours of administration, arterial blood pressure remained 12% lower than the control level.[1]

Synonyms	BMS182874, BMS-182874
Molecular Weight	345.42
Formula	C17H19N3O3S
CAS No.	153042-42-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Abdullaha M, et al. Methoxy-naphthyl-Linked N-Benzyl Pyridinium Styryls as Dual Cholinesterase Inhibitors: Design, Synthesis, Biological Evaluation, and Structure-Activity Relationship. ACS Omega. 2023;8(20):17591-17608. 2. Holm P, et al. The ETA receptor antagonist, BMS-182874, reduces acute hypoxic pulmonary hypertension in pigs in vivo. Cardiovasc Res. 1998;37(3):765-771. 3. Webb ML, et al. BMS-182874 is a selective, nonpeptide endothelin ETA receptor antagonist. J Pharmacol Exp Ther. 1995;272(3):1124-1134. 4. Chong S, et al. Pharmacokinetics and metabolism of endothelin receptor antagonist: contribution of kidneys in the overall in vivo N-demethylation. Arch Pharm Res. 2003;26(1):89-9 5. Park JB, et al. ET(A) receptor antagonist prevents blood pressure elevation and vascular remodeling in aldosterone-infused rats. Hypertension. 2001;37(6):1444-1449.

Related compound libraries

This product is contained In the following compound libraries：

Membrane Protein-targeted Compound Library GPCR Compound Library Bioactive Compounds Library Max Bioactive Compound Library

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Related compounds with same targets

Endothelin 1 (swine, human) acetate Avosentan Aminaftone SB-209670 Ro 46-2005 Edonentan Ambrisentan Sitaxsentan

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Keywords

BMS 182874 153042-42-3 GPCR/G Protein Endothelin Receptor BMS182874 BMS-182874 inhibitor inhibit

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