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製品番号: HY-150790

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BMS-986141

Name: BMS-986141
Brand: MedChemExpress
SKU: HY-150790
Price: 780.00 USD
Availability: InStock
Rating: 5 (1 reviews)

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Based on 1 Customer Validation

BMS-98614 is an orally active, selective thrombin receptor protease-activated receptor-4 (PAR-4) antagonist with an IC₅₀ value of 0.4 nM. BMS-98614 has excellent antithrombotic effect.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

純度 : 98.15%
CAS 番号: 1478711-48-6
分子式: C₂₇H₂₃N₅O₅S₂
分子量:561.63

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

BMS-986141 構造式

CAS 番号: 1478711-48-6

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
- 臨床実験
化学情報
溶剤 & 溶解度
- 体外
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

BMS-98614 is an orally active, selective thrombin receptor protease-activated receptor-4 (PAR-4) antagonist with an IC₅₀ value of 0.4 nM. BMS-98614 has excellent antithrombotic effect^[1]^[2].

IC₅₀ & Target

^[1]

PAR4

.4 nM (IC₅₀)

Protease Activated Receptor (PAR) アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
Platelet	IC₅₀	>1000 nM Compound: 49; BMS-986141	Antiplatelet activity against collagen agonist peptide-induced human platelet assessed as inhibition of platelet aggregation Antiplatelet activity against collagen agonist peptide-induced human platelet assessed as inhibition of platelet aggregation	[PMID: 35729784]
Platelet	IC₅₀	>1000 nM Compound: 49; BMS-986141	Antiplatelet activity against PAR1 agonist peptide-induced human platelet assessed as inhibition of platelet aggregation Antiplatelet activity against PAR1 agonist peptide-induced human platelet assessed as inhibition of platelet aggregation	[PMID: 35729784]
Platelet	IC₅₀	>1000 nM Compound: 49; BMS-986141	Antiplatelet activity against U46619 agonist peptide-induced human platelet assessed as inhibition of platelet aggregation Antiplatelet activity against U46619 agonist peptide-induced human platelet assessed as inhibition of platelet aggregation	[PMID: 35729784]
Platelet	IC₅₀	2.1 nM Compound: 49; BMS-986141	Antiplatelet activity in human platelet-rich plasma assessed as inhibition of gamma thrombin induced platelet aggregation preincubated for 5 mins followed by gamma thrombin addition and measured upto 15 mins by plate reader assay Antiplatelet activity in human platelet-rich plasma assessed as inhibition of gamma thrombin induced platelet aggregation preincubated for 5 mins followed by gamma thrombin addition and measured upto 15 mins by plate reader assay	[PMID: 35729784]
Platelet	IC₅₀	2.2 nM Compound: 49; BMS-986141	Antiplatelet activity against PAR4 agonist peptide-induced human platelet assessed as inhibition of platelet aggregation Antiplatelet activity against PAR4 agonist peptide-induced human platelet assessed as inhibition of platelet aggregation	[PMID: 35729784]
Platelet	IC₅₀	>1000 nM Compound: 49; BMS-986141	Antiplatelet activity against ADP agonist peptide-induced human platelet assessed as inhibition of platelet aggregation Antiplatelet activity against ADP agonist peptide-induced human platelet assessed as inhibition of platelet aggregation	[PMID: 35729784]

体外実験

BMS-986141 (compound 49) (0-1 μM) inhibits platelet aggregation induced by PAR4 agonist peptide with an IC₅₀ value of 2.2 nM^[1].

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

体内実験

BMS-986141 (compound 49) shows a slight but significant prolongation of KBT (kidney bleeding time) and demonstrates excellent anti-thrombotic efficacy at 0.5 mg/kg in cynomolgus monkey^[1]^[2].

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

Animal Model:

Monkey arterial thrombosis (AT) and mesenteric bleeding time (MBT) models^[2]
Dosage:

0.05, 0.1, 0.5 mg/kg
Administration:

p.o., 2 hours
Result:

Inhibited PAR4-AP-induced platelet aggregation in human and monkey blood with IC50 of 1.8 and 1.3 nM, respectively.
Reduced the thrombus weight by 36%, 63% and 88% at concentrations of 0.05, 0.1 and 0.5 mg/kg, respectively in AT model.
Increased MBT by 1.2 times.

Animal Model:

Rat, dog and monkey^[1]
Dosage:

0.5, 1, 2 mpk
Administration:

i.v., 0.5 mpk, 10 min or p.o., 2 mpk for rat, 1 mpk for dog and monkey
Result:

The pharmacokinetic parameters of BMS-986141 (compound 49)

Parameters rat dog monkey

t_1/2(h) 3.7 ± 0.4 13 75 ± 12

CL (mL/min/kg) 14.3 ± 0.4 8.5 12 ± 2

Vss(L/kg) 2.7 ± 0.3 2.7 14 ± 5

F (%) 31 25 36

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991			2011-05	PHASE1

化学情報

CAS 番号 1478711-48-6
性状 Solid
分子量 561.63
分子式 C₂₇H₂₃N₅O₅S₂
Color White to off-white
SMILES

O=C(N(C)C)C1=CC=C(C2=NC(COC3=C4C=C(C5=CN6C(SC(OC)=N6)=N5)OC4=CC(OC)=C3)=CS2)C=C1
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

DMF : 8.33 mg/mL (14.83 mM; ultrasonic and warming and heat to 60°C)

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

1.7805 mL

8.9027 mL

17.8053 mL

5 mM

0.3561 mL

1.7805 mL

3.5611 mL

10 mM

0.1781 mL

0.8903 mL

1.7805 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (277 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
COA (2659 KB)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[1]. E Scott Priestley, et al. Discovery of Two Novel Antiplatelet Clinical Candidates (BMS-986120 and BMS-986141) That Antagonize Protease-Activated Receptor 4. J Med Chem. 2022 Jul 14;65(13):8843-8854. [Content Brief]

[2]. P Wong, et al. Favorable therapeutic index of an orally-active small-molecule antagonist of the platelet protease-activated receptor-4, BMS-986141, compared with the P2Y12 antagonist ticagrelor in cynomolgus monkeys. European Heart Journal, Volume 41, Issue Supplement_2, November 2020.

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

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. 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
DMF	1 mM	1.7805 mL	8.9027 mL	17.8053 mL	44.5133 mL
	5 mM	0.3561 mL	1.7805 mL	3.5611 mL	8.9027 mL
	10 mM	0.1781 mL	0.8903 mL	1.7805 mL	4.4513 mL

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
- 臨床実験
化学情報
溶剤 & 溶解度
- 体外実験
純度とドキュメンテーション
参考文献

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Parameters	rat	dog	monkey
t_1/2(h)	3.7 ± 0.4	13	75 ± 12
CL (mL/min/kg)	14.3 ± 0.4	8.5	12 ± 2
Vss(L/kg)	2.7 ± 0.3	2.7	14 ± 5
F (%)	31	25	36

BMS-986141

Protease Activated Receptor (PAR) アイソフォーム固有の製品をすべて表示

生物活性

製品説明

IC50 & Target

Cellular Effect

体外実験

体内実験

臨床実験

化学情報

溶剤 & 溶解度

体外:

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

BMS-986141 関連分類

HY-150790 関連分類

Bioz

Keywords

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IC₅₀ & Target