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製品番号: HY-110391

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BX-513

(別名: VUF 2274)

BX-513 is a highly potent and selective CCR1 antagonist. BX-513 effectively inhibits the binding of radiolabeled MIP-1α and RANTES to CCR1, with K_i values of 40 nM and 60 nM, respectively. BX-513 suppresses MIP-1α-induced extracellular acidification, MIP-1α- and RANTES-induced intracellular calcium mobilization, as well as MIP-1α- and RANTES-induced migration of peripheral blood mononuclear cells. BX-513 can be used for the research of rheumatoid arthritis and multiple sclerosis.

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。
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CAS 番号: 193542-65-3
分子式: C₂₈H₂₉ClN₂O
分子量:445.00

保管条件:

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

BX-513 構造式

CAS 番号: 193542-65-3

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生物活性
- 製品説明
- Cellular Effect
- 体外実験
- 臨床実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
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関連分類
Bioz

生物活性

製品説明

CCR 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
CHO	IC₅₀	0.63 μM Compound: 23	Inhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cells Inhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cells	[PMID: 12166951]
CHO	IC₅₀	9 μM Compound: 23	Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells	[PMID: 12166951]
COS-7	EC₅₀	3.2 μM Compound: 1 table-1	Effective concentration against US28-mediated inositol phosphate production in COS-7 cells Effective concentration against US28-mediated inositol phosphate production in COS-7 cells	[PMID: 16190772]
COS-7	IC₅₀	9.3 μM Compound: 1 table-1	Inhibitory concentration against chemokine receptor US28 expressed in COS-7 cells using [125I]-CCL5 Inhibitory concentration against chemokine receptor US28 expressed in COS-7 cells using [125I]-CCL5	[PMID: 16190772]
HEK293	EC₅₀	4.5 μM Compound: VUF2274	Inverse agonist activity at HCMV TB40/E US28 expressed in human HEK cells assessed as Elk-1 activation preincubated for 1 hrs measured after 20 to 24 hrs by luciferase reporter gene assay Inverse agonist activity at HCMV TB40/E US28 expressed in human HEK cells assessed as Elk-1 activation preincubated for 1 hrs measured after 20 to 24 hrs by luciferase reporter gene assay	[PMID: 21784633]
HEK293	IC₅₀	2.5 μM Compound: 6s	Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor	[PMID: 10579830]
HEK-293T	EC₅₀	>10 μM Compound: VUF2274	Allosteric modulatory activity at FLAG-tagged human cytomegalovirus US28 receptor delta300 mutant expressed in HEK293T cells by PathDetectElk1 assay Allosteric modulatory activity at FLAG-tagged human cytomegalovirus US28 receptor delta300 mutant expressed in HEK293T cells by PathDetectElk1 assay	[PMID: 25052428]
HEK-293T	EC₅₀	4.5 μM Compound: VUF2274	Allosteric modulatory activity at FLAG-tagged wild type human cytomegalovirus US28 receptor expressed in HEK293T cells by PathDetectElk1 assay Allosteric modulatory activity at FLAG-tagged wild type human cytomegalovirus US28 receptor expressed in HEK293T cells by PathDetectElk1 assay	[PMID: 25052428]

体外実験

BX-513 (Compound 1) (30-1000 nM) dose-dependently inhibits MIP-1α-induced extracellular acidification in THP-1 cells, with an IC₅₀ of 124 nM, and also suppresses RANTES-induced acidification in these cells^[1].
BX-513 (100-1000 nM) inhibits CCR1-expressing HEK 293 cells in a dose-dependent manner, with an IC₅₀ of approximately 200 nM. This compound has no intrinsic agonist activity, exerts reversible inhibitory effects, and also inhibits RANTES-induced intracellular Ca²⁺ mobilization in these cells^[1].
BX-513 (20-2000 nM) dose-dependently inhibits MIP-1α- and RANTES-induced chemotaxis of human peripheral blood mononuclear cells (PBMCs), without affecting migration induced by other chemokines^[1].

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

臨床実験

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

化学情報

CAS 番号 193542-65-3
分子量 445.00
分子式 C₂₈H₂₉ClN₂O
SMILES

N#CC(C=1C=CC=CC1)(C=2C=CC=CC2)CCCN3CCC(O)(C4=CC=C(Cl)C=C4)CC3
別名

VUF 2274
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

取扱説明書 (2659 KB)

参考文献

[1]. Hesselgesser J, et al. Identification and characterization of small molecule functional antagonists of the CCR1 chemokine receptor. J Biol Chem. 1998;273(25):15687-15692. [Content Brief]

Calculators

モル濃度計算機

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

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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.

MOQ

Minimum order quantity

100 mg

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生物活性
- 製品説明
- 体外実験
- 臨床実験
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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BX-513

CCR 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

BX-513 関連分類

HY-110391 関連分類