239825

AMD3100

InSolution, ≥98%, 50 mM aqueous solution, CXCR4 antagonist I

• 同義詞: InSolution CXCR4 Antagonist I, AMD3100, 1,1ʹ(1,4-Phenylenebis(methylene))-bis-1,4,8,11-tetraazacyclotetradecane, 8HCl, 4H₂O, 1,4-bis((1,4,8,11-Tetraazacyclotetradecan-1-yl)methyl)benzene, 8HCl, 4H₂O
• 經驗公式（希爾表示法）: C₂₈H₅₄N₈ · 8HCl · 4H₂O
• CAS號碼: 155148-31-5
• 分子量：: 866.53
• MDL號碼: MFCD04974488
• 分類程式碼代碼: 51111800
• NACRES: NA.77

屬性

• 品質等級: 100
• 化驗: ≥98% (HPLC)
• 形狀: liquid
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; avoid repeated freeze/thaw cycles; protect from light
• 運輸包裝: dry ice
• 儲存溫度: −70°C
• SMILES 字串: Cl.Cl.Cl.Cl.Cl.Cl.Cl.Cl.N3(CCNCCCNCCNCCC3)Cc1ccc(cc1)CN2CCNCCCNCCNCCC2
• InChI: 1S/C28H54N8.8ClH/c1-9-29-15-17-31-13-3-21-35(23-19-33-11-1)25-27-5-7-28(8-6-27)26-36-22-4-14-32-18-16-30-10-2-12-34-20-24-36;;;;;;;;/h5-8,29-34H,1-4,9-26H2;8*1H
• InChI 密鑰: UEUPDYPUTTUXLJ-UHFFFAOYSA-N

描述

一般說明

A symmetrical bicyclam compound that antagonizes CXCL12 (SDF1) binding to CXCR4 (IC₅₀ = 108 and 245 nM using rat and human CXCR4, respectively) and inhibits SDF1-induced Ca²⁺ flux (by 100% at 100 ng/ml in SUP-T1 and THP-1 cultures) as well as CXCR4-, but not CCR5-, mediated HIV infection (IC₅₀ = 200 nM), while enhancing the binding of SDF1 to CXCR7 (by ~60% at 1 mM with CXCR7-expressing HEK293T cells) and SDF1-induced β-arrestin recruitment to CXCR7 (EC₅₀ = 6.48 and 11.8 nM, in the presence and absence of 10 µM AMD3100, respectively). Administration AMD3100 via intravenous infusion is also reported to result in hematopoietic stem cell mobilization in humans, dogs, and mice in vivo. Exhibits no inhibitory effects against chemokine-induced signaling via CXCR1/2/3 or CCR1/2/3/4/5/6/7/8/9.

生化／生理作用

Cell permeable: yes

Primary Target
CXCR4

Reversible: yes

包裝

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

外觀

A 50 mM (15 mg/308 µL) solution of CXCR4 Antagonist I, AMD3100 (Cat. No. 239820) in H₂O.

重構

Following initial thaw, aliquot and freeze (-70°C). Aliquots are stable for up to 1 year at -70°C.

其他說明

Kalatskaya, I., et al. 2009. Mol. Pharmacol.77, 1240.
Pitchford, S.C., et al. 2009. Cell Stem Cell4, 62.
De Clercq, E. 2009. Biochem. Pharmacol.77, 1655.
Thoma, G., et al. 2008. J. Med. Chem.51, 7915.
De Clercq, E. 2000. Mol. Pharmacol.57, 833.

法律資訊

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全資訊

• 儲存類別代碼: 10 - Combustible liquids
• 水污染物質分類（WGK）: WGK 3