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製品番号: HY-13829

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BMS-585248

BMS-585248 is a potent, third-generation HIV-1 attachment inhibitor with a promising initial in vitro and in vivo pharmacokinetic profile.

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CAS 番号: 619331-12-3
分子式: C₂₂H₁₈FN₇O₃
分子量:447.42

保管条件:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (276 KB)

BMS-585248 構造式

CAS 番号: 619331-12-3

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Fluorescent Dye

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

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

生物活性

製品説明

BMS-585248 is a potent, third-generation HIV-1 attachment inhibitor with a promising initial in vitro and in vivo pharmacokinetic profile^[1].

IC₅₀ & Target

HIV-1

HIV 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
HeLa	CC₅₀	>300 μM Compound: 12m, BMS-585428	Cytotoxicity against human HeLa cells Cytotoxicity against human HeLa cells	[PMID: 23360431]
MT2	EC₅₀	0.8 nM Compound: 12m, BMS-585428	Antiviral activity against HIV1 BRU infected in MT2 cells after 4 to 5 days by reverse transcriptase assay in absence of human serum Antiviral activity against HIV1 BRU infected in MT2 cells after 4 to 5 days by reverse transcriptase assay in absence of human serum	[PMID: 23360431]
MT2	EC₅₀	0.87 nM Compound: 12m, BMS-585428	Antiviral activity against X4-tropic HIV1 LAI infected in MT2 cells Antiviral activity against X4-tropic HIV1 LAI infected in MT2 cells	[PMID: 23360431]
MT2	EC₅₀	1.32 nM Compound: 12m, BMS-585428	Antiviral activity against X4-tropic HIV1 NL4-3 infected in MT2 cells Antiviral activity against X4-tropic HIV1 NL4-3 infected in MT2 cells	[PMID: 23360431]
MT2	EC₅₀	2.3 nM Compound: 12m, BMS-585428	Antiviral activity against HIV1 BRU infected in MT2 cells after 4 to 5 days by reverse transcriptase assay in presence of human serum Antiviral activity against HIV1 BRU infected in MT2 cells after 4 to 5 days by reverse transcriptase assay in presence of human serum	[PMID: 23360431]
MT2	EC₅₀	5.17 nM Compound: 12m, BMS-585428	Antiviral activity against X4-tropic HIV1 MN infected in MT2 cells Antiviral activity against X4-tropic HIV1 MN infected in MT2 cells	[PMID: 23360431]
U-87MG ATCC	IC₅₀	<5 nM Compound: 29	Antiviral activity against HIV1 pseudovirus in U87 cells expressing CD4 and CCR5 after 72 hrs by M33 pseudotyped assay Antiviral activity against HIV1 pseudovirus in U87 cells expressing CD4 and CCR5 after 72 hrs by M33 pseudotyped assay	[PMID: 18052117]
U-87MG ATCC	CC₅₀	>40000 nM Compound: 29	Cytotoxicity against human U87 cells expressing CD4 and CXCR4 Cytotoxicity against human U87 cells expressing CD4 and CXCR4	[PMID: 18052117]
U-87MG ATCC	CC₅₀	>40000 nM Compound: 3	Cytotoxicity against human U87 cells coexpressing CD4, CxCR4 receptors after 72 hrs Cytotoxicity against human U87 cells coexpressing CD4, CxCR4 receptors after 72 hrs	[PMID: 19534463]

体内実験

BMS-585248 (intravenous (1 mg/kg) and oral (5-200 mg/kg); once) has a good pharmacokinetic profile, with AUC values of 3220 nM·h and 8064 nM·h after IV (1 mg/kg) and oral (5 mg/kg) administration in male rats, respectively^[1].

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

Animal Model:

Male rats^[1]
Dosage:

5, 15, and 200 mg/kg
Administration:

Orally, once (Pharmacokinetic Analysis)
Result:

Pharmacokinetic Parameters of BMS-585248 in male rats^[1].

PO

Dose (mg/kg) 15 75 200

C_max (μM) 6.6 8.4 11

AUC_tot (μM·h) 42 115 145

化学情報

CAS 番号 619331-12-3
分子量 447.42
分子式 C₂₂H₁₈FN₇O₃
SMILES

O=C(N1CCN(C(C2=CC=CC=C2)=O)CC1)C(C3=CNC4=C3C(F)=CN=C4N5N=NC=C5)=O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

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 (276 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]. Regueiro-Ren A, et al. Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment 13. Synthesis and profiling of a novel amminium prodrug of the HIV-1 attachment inhibitor BMS-585248. J Med Chem. 2013 Feb 28;56(4):1670-6. [Content Brief]

Calculators

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)

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.

Keywords

MOQ

Minimum order quantity

100 mg

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

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	PO
Dose (mg/kg)	15	75	200
C_max (μM)	6.6	8.4	11
AUC_tot (μM·h)	42	115	145

BMS-585248

HIV アイソフォーム固有の製品をすべて表示

生物活性

化学情報

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

BMS-585248 関連分類

HY-13829 関連分類