Referencia número: HY-118497

BMS 182874

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BMS 182874 is an orallyactive, highly selective endothelin receptor (ET_A receptor) antagonist, with IC₅₀ value of 0.150 μM, K_i 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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Pureza: 99.85%
No. CAS: 153042-42-3
Fòrmula: C₁₇H₁₉N₃O₃S
Peso molecular:345.42

Almacenamiento:

4°C, protect from light

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

BMS 182874 Chemical Structure

No. CAS: 153042-42-3

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvente y solubilidad
- In Vitro
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target^[1]

ET_A

0.15 μM (IC₅₀)

ET_A

0.055 μM (Ki)

Ver todos los productos específicos de isoformas Endothelin Receptor :

ET_A
ET_B

Cellular Effect

Cell Line	Type	Value	Description	References
A10	IC₅₀	0.15 μM Compound: 11	Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells	[PMID: 8308857]
A10	IC₅₀	570 nM Compound: 11	Antagonism of ET-1 induced increase in intracellular Ca+2 in vsm-A10 cells Antagonism of ET-1 induced increase in intracellular Ca+2 in vsm-A10 cells	[PMID: 8308857]

In Vitro

BMS-182874 (dimethyla minoanalogue 11) is an antagonist of the ET_A ,with IC₅₀ value of 0.150 μM and K_i 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.

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.

Chemical Information

No. CAS 153042-42-3
Appearance Solid
Peso molecular 345.42
Fòrmula C₁₇H₁₉N₃O₃S
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
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

4°C, protect from light

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

Solvente y solubilidad

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.8950 mL

14.4751 mL

28.9503 mL

5 mM

0.5790 mL

2.8950 mL

5.7901 mL

10 mM

0.2895 mL

1.4475 mL

2.8950 mL

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.

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (276 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[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 May 9;8(20):17591-17608. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Anti-Cardiovascular Disease Compound Library

Orally Active Compound Library

Neurotransmitter Receptor Compound Library

Angiogenesis-Related Compound Library

Human Metabolite Library

Coagulation and Anti-coagulation Compound Library

Pain-Related Compound Library

Antihypertensive Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Lactylation Compound Library

GPCR/G Protein Compound Library

Ver todos los productos específicos de isoformas Endothelin Receptor

Actividad biológica

Chemical Information

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

BMS 182874

Anti-Cardiovascular Disease Compound Library

Orally Active Compound Library

Neurotransmitter Receptor Compound Library

Angiogenesis-Related Compound Library

Human Metabolite Library

Coagulation and Anti-coagulation Compound Library

Pain-Related Compound Library

Antihypertensive Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Lactylation Compound Library

GPCR/G Protein Compound Library

Ver todos los productos específicos de isoformas Endothelin Receptor

Actividad biológica

Chemical Information

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

BMS 182874 Related Classifications

HY-118497 Related Classifications