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BMY 7378 dihydrochloride

Catalog No. T3046 CAS 21102-95-4

Synonyms: BMY7378 HCl

BMY 7378 dihydrochloride (BMY7378 HCl) , α1D-adrenergic receptor antagonist, is a weak partial agonist/antagonist of 5-HT1A receptor.

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BMY 7378 dihydrochloride Chemical Structure

BMY 7378 dihydrochloride, CAS 21102-95-4

Pack Size	Availability	Price/USD
5 mg	In stock	$ 37.00
10 mg	In stock	$ 50.00
25 mg	In stock	$ 81.00
50 mg	In stock	$ 103.00
1 mL * 10 mM (in DMSO)	In stock	$ 50.00

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Purity: 99.08%

Purity: 98.65%

Purity: 97.67%

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Storage & Solubility Information

Description	BMY 7378 dihydrochloride (BMY7378 HCl) , α1D-adrenergic receptor antagonist, is a weak partial agonist/antagonist of 5-HT1A receptor.
Targets&IC50	5-HT1A:8.3(pIC50), α1D-adrenoceptor:8.2(pKi), 5-HT1C:6.4(pIC50), D2 receptor:7.4(pIC50), α2C-adrenoceptor:6.54(pKi)
Kinase Assay	Phosphatase activities are determined on immunoprecipitates of the phosphatases. Briefly, 2×106 K562 cells are treated for 18 hr with Salubrinal (20 μM), PSI (10 nM), the combination of both drugs or okadaic acid (100 nM). After washing with PBS, cells are lysed for 15 min on ice either in PP1LB (for determination of PP1γ-activity; 20 mM Tris-HCl, pH 7.5, 1% Triton X-100, 10% glycerol, 132 mM NaCl, Roche complete protease inhibitor ) or in RIPA (for PP2A), supplemented with Roche complete protease inhibitor). Cell lysates containing 500 μg (PP1γ) or 300 μg (PP2A) protein are immunoprecipitated overnight at 4°C with 2-3 μg of the appropriate antibodies and then incubated with Protein A-Sepharose. Immunoprecipitates are washed three times in lysis buffer, followed by resuspension in phosphatase assay buffer (PP2A: 20 mM Tris-HCl, pH7.5, 0.1 mM CaCl2; PP1γ: 50 mM Tris HCl pH 7.0, 0.2 mM MnCl2, 0.1 mM CaCl2, 125 μg/mL BSA, 0.05% Tween 20), supplemented with 100 μM 6,8-difluoro-4-methyl-umbelliferyl phosphate (DiFMUP). Precipitates are allowed to react with substrate for 1 hr at 37°C on an Eppendorf Thermoshaker, centrifuged and DiFMU fluorescence is measured on a BioTek Lambda Fluoro 320 microplate reader (360 nmex/460 nmem). Phosphatase activities are given as percent change relative to the control (DMSO treated cells)[1].

Synonyms	BMY7378 HCl
Molecular Weight	458.42
Formula	C22H33Cl2N3O3
CAS No.	21102-95-4

Storage

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

Solubility Information

Ethanol: 16 mg/mL (34.9 mM)

DMSO: 85 mg/mL (185.4 mM)

H2O: 84 mg/mL (183.2 mM)

References and Literature

1. Cleary L, et al. Auton Autacoid Pharmacol, 2005, 25(4), 135-141. 2. Goetz AS, et al. Eur J Pharmacol, 1995, 272(2-3), R5-6. 3. Greuel JM, et al. Eur J Pharmacol, 1992, 211(2), 211-219. 4. Sharp T, et al. Eur J Pharmacol, 1990, 176(3), 331-40.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Neurodegenerative Disease Compound Library GPCR Compound Library Neurotransmitter Receptor Compound Library Anti-Hypertension Compound Library Adrenergic Receptor-Targeted Compound Library Anti-Cardiovascular Disease Compound Library Angiogenesis related Compound Library Bioactive Compound Library Serotonin Receptor-Targeted Compound Library

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Keywords

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