BMS-566419
Based on 1 Customer Validation
BMS-566419 is an orally active IMPDH inhibitor with an IC50 of 91 nM against human IMPDH I and 68 nM against human IMPDH II. BMS-566419 exerts anti-heart transplant rejection and anti-renal fibrosis effects, and inhibits the expression of MCP-1, TGF-β1 as well as antibody production. BMS-566419 can be used in research on renal fibrosis and organ transplantation.
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- Purity: 99.68%
- CAS No.: 566161-24-8
- 화학식: C28H30FN5O2
- 분자량:487.57
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CCRF-CEM | IC50 |
0.77 μM
Compound: 4m
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Inhibition of CEM cell proliferation
Inhibition of CEM cell proliferation
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[PMID: 17585753] |
| PBMC | IC50 |
0.22 μM
Compound: 4m
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Inhibition of T cell proliferation in PBMC cells
Inhibition of T cell proliferation in PBMC cells
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[PMID: 17585753] |
BMS-566419 (48 h) inhibits Concanavalin A (HY-P2149)-stimulated splenic T cell proliferation in Lewis rats, with an IC50 of 320 nM[1].
BMS-566419 (48 h) inhibits the proliferation of LPS (HY-D1056)-stimulated B cells from the spleen of Lewis rats, with an IC50 of 230 nM[1].
BMS-566419 (72 h) inhibits allogeneic antigen-specific proliferation of T cells from Lewis rats in mixed lymphocyte reactions, with an IC50 of 95 nM[1].
BMS-566419 (10-1000 nM; 72 h) inhibits IgM production in LPS-stimulated splenic B cells from Lewis rats in vitro, with an IC50 of 170 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
BMS-566419 (30-60 mg/kg; p.o.; 4 days) significantly inhibits T-cell-independent anti-DNP IgM antibody production in rats, with a maximum inhibition rate of over 95%[1].
BMS-566419 (60 mg/kg; p.o.; 7 days) significantly inhibits the production of alloantigen-specific IgM and IgG1/2a antibodies in rats, with inhibition rates of 70% and 96%, respectively[1].
BMS-566419 (30-60 mg/kg; p.o.; 14 days) exerts a dose-dependent inhibitory effect on renal fibrosis induced by UUO in rats[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague Dawley (7-week-old male, unilateral ureteral obstruction model)[2]
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Dosage:30 mg/kg; 60 mg/kg
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Administration:p.o.; daily; 14 days
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Result:Had a dose-dependent suppressive effect on renal interstitial fibrosis in male Sprague Dawley rats with unilateral ureteral obstruction (UUO) model.
Significantly reduced the hydroxyproline concentration, collagen type Ⅰ mRNA, MCP-1 mRNA and TGF-β1 mRNA expression in renal tissues.
Chemical Information
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CAS No. 566161-24-8
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Appearance Solid
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분자량 487.57
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화학식 C28H30FN5O2
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Color Light yellow to yellow
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SMILES
O=C1C2=CC(F)=C(C(NC(C)(C3=CN=C(N4CCN(CC)CC4)C=C3)C)=O)C=C2NC5=CC=CC=C15
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 12.5 mg/mL (25.64 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (272 KB)
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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)
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Handling Instructions (2659 KB)
References
[1]. Nakanishi T, et al. Effect of the inosine 5'-monophosphate dehydrogenase inhibitor BMS-566419 on rat cardiac allograft rejection. Int Immunopharmacol. 2010;10(1):91-97. [Content Brief]
[2]. Nakanishi T, et al. Effect of the inosine 5'-monophosphate dehydrogenase inhibitor BMS-566419 on renal fibrosis in unilateral ureteral obstruction in rats. Int Immunopharmacol. 2010;10(11):1434-1439. [Content Brief]
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. 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 | 2.0510 mL | 10.2549 mL | 20.5099 mL | 51.2747 mL |
| 5 mM | 0.4102 mL | 2.0510 mL | 4.1020 mL | 10.2549 mL | |
| 10 mM | 0.2051 mL | 1.0255 mL | 2.0510 mL | 5.1275 mL | |
| 15 mM | 0.1367 mL | 0.6837 mL | 1.3673 mL | 3.4183 mL | |
| 20 mM | 0.1025 mL | 0.5127 mL | 1.0255 mL | 2.5637 mL | |
| 25 mM | 0.0820 mL | 0.4102 mL | 0.8204 mL | 2.0510 mL |
BMS-566419 Related Classifications
HY-110217 Related Classifications
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