2. GPCR/G Protein
  3. Endothelin Receptor
  4. BMS 182874

BMS 182874 is an orallyactive, highly selective endothelin receptor (ETA receptor) antagonist, with IC50 value of 0.150 μM, Ki of 0.055 μM. BMS 182874 reduces the arterial pressure of Deoxycorticosterone acetate (HY-B1472) induced hypertension model in rats, and can be used for cardiovascular disease research.

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BMS 182874 Chemical Structure

BMS 182874 Chemical Structure

CAS No. : 153042-42-3

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Based on 1 publication(s) in Google Scholar

BMS 182874 Related Antibodies

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Description

BMS 182874 is an orallyactive, highly selective endothelin receptor (ETA receptor) antagonist, with IC50 value of 0.150 μM, Ki of 0.055 μM. BMS 182874 reduces the arterial pressure of Deoxycorticosterone acetate (HY-B1472) induced hypertension model in rats, and can be used for cardiovascular disease research[1].

IC50 & Target[1]

ETA

0.15 μM (IC50)

ETA

0.055 μM (Ki)

In Vitro

BMS-182874 (dimethyla minoanalogue 11) is an antagonist of the ETA ,with IC50 value of 0.150 μM and Ki of 0.055 μM in vsm-A10 cells, and with a KB value of 0.520 μM in rabbit carotid artery rings[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

BMS 182874 Related Antibodies
In Vivo

BMS 182874 (100 μM/kg, p.o.; a single oral) makes arterial pressure slowly fell by 25% from a control level. After dosing for 12 and 24 h makes arterial pressure is still 12% below the control level[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Kidney Deoxycorticosterone acetate -salt hypertensive rats[1]
Dosage: 100 μM/kg
Administration: Oral gavage (p.o.); Intravenous injection (i.v.)
Result: Made arterial pressure slowly fell by 25% from a control level. After dosing for 12 and 24 h, makes arterial pressure is still 12% below the control level.
Molecular Weight

345.42

Formula

C17H19N3O3S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=S(C1=C2C=CC=C(C2=CC=C1)N(C)C)(NC3=C(C(C)=NO3)C)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (361.88 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8950 mL 14.4751 mL 28.9503 mL
5 mM 0.5790 mL 2.8950 mL 5.7901 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8950 mL 14.4751 mL 28.9503 mL 72.3757 mL
5 mM 0.5790 mL 2.8950 mL 5.7901 mL 14.4751 mL
10 mM 0.2895 mL 1.4475 mL 2.8950 mL 7.2376 mL
15 mM 0.1930 mL 0.9650 mL 1.9300 mL 4.8250 mL
20 mM 0.1448 mL 0.7238 mL 1.4475 mL 3.6188 mL
25 mM 0.1158 mL 0.5790 mL 1.1580 mL 2.8950 mL
30 mM 0.0965 mL 0.4825 mL 0.9650 mL 2.4125 mL
40 mM 0.0724 mL 0.3619 mL 0.7238 mL 1.8094 mL
50 mM 0.0579 mL 0.2895 mL 0.5790 mL 1.4475 mL
60 mM 0.0483 mL 0.2413 mL 0.4825 mL 1.2063 mL
80 mM 0.0362 mL 0.1809 mL 0.3619 mL 0.9047 mL
100 mM 0.0290 mL 0.1448 mL 0.2895 mL 0.7238 mL
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BMS 182874 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BMS 182874153042-42-3BMS182874BMS-182874Endothelin ReceptorEndothelin receptor antagonistETA AntagonisthypertensionInhibitorinhibitorinhibit

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