BMS-566419

Name: BMS-566419
Brand: MedChemExpress
SKU: HY-110217
Rating: 4.5 (1 reviews)

Cat. No.: HY-110217 Purity: 99.68%: Data Sheet
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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.

For research use only. We do not sell to patients.

BMS-566419 Chemical Structure

CAS No. : 566161-24-8

Size	Stock	Quantity
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
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100 mg	Get quote

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Based on 1 publication(s) in Google Scholar

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Description

Cellular Effect

Cell Line	Type	Value	Description	References
CCRF-CEM	IC₅₀	0.77 μM Compound: 4m	Inhibition of CEM cell proliferation Inhibition of CEM cell proliferation	[PMID: 17585753]
PBMC	IC₅₀	0.22 μM Compound: 4m	Inhibition of T cell proliferation in PBMC cells Inhibition of T cell proliferation in PBMC cells	[PMID: 17585753]

In Vitro

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.

In Vivo

BMS-566419 (10-60 mg/kg; p.o.; 14 days) significantly prolongs the median survival time of rat heart transplants at doses of 30 and 60 mg/kg, to 10 days and 18 days respectively, and exhibits better efficacy when co-administered with Tacrolimus (HY-13756)^[1].
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.

Animal Model:	Sprague Dawley (7-week-old male, unilateral ureteral obstruction model)^[2]
Dosage:	30 mg/kg; 60 mg/kg
Administration:	p.o.; daily; 14 days
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.

Molecular Weight

487.57

Formula

C₂₈H₃₀FN₅O₂

CAS No.

566161-24-8

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C2=CC(F)=C(C(NC(C)(C3=CN=C(N4CCN(CC)CC4)C=C3)C)=O)C=C2NC5=CC=CC=C15

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.0510 mL	10.2549 mL	20.5099 mL
5 mM	0.4102 mL	2.0510 mL	4.1020 mL
10 mM	0.2051 mL	1.0255 mL	2.0510 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. 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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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.68%

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Data Sheet (272 KB) SDS (254 KB)

COA (245 KB) HNMR (138 KB) RP-HPLC (145 KB)

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

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

Inflammation/Immunology

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-566419566161-24-8BMS566419BMS 566419IMPDHInosine-5’-monophosphate dehydrogenaseB cellsMCP-1fibrosiscardiac allograft rejectionInhibitorinhibitorinhibit

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BMS-566419

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