5.00507

CXCR4 Antagonist IV, TF14016

• 別名: CXCR4 Antagonist IV, TF14016, Fusin Antagonist IV
• 実験式（ヒル表記法）: C₁₀₁H₁₄₅FN₃₄O₁₈S₂ · xH₂O
• 分子量: 2206.58 (anhydrous basis)
• UNSPSCコード: 51111800
• NACRES: NA.77

特性

• アッセイ: ≥95% (HPLC)
• 品質水準: 100
• フォーム: solid
• 有効性: 0.9 nM IC₅₀
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: white
• 溶解性: H₂O: 100 mg/mL
• 保管温度: −20°C

詳細

詳細

A 14-aa internally disulfide-bonded peptide that potently competes against SDF-1α/CXCL12 for CXCR4 binding (IC₅₀ = 0.91 nM; [SDF-1] = 100 nM) and protects MT-4 cells against X4-HIV strain HIV-1_IIIB infection (EC₅₀ = 4 nM in 5 d; MOI = 0.01) with no significant cytotoxicity (CC₅₀ = 56 µM; 5 d). Inhibits SDF-1-induced Ca²⁺ mobilization (IC₅₀ = 4.5 nM; [SDF-1] = 30 nM; CXCR4-expressing CHO cells) in vitro and effectively prevents CXCR4-dependent 5BC-5 metastasis in NK-depleted SCID mice in vivo (10 mg/kg i.p.) in vivo.

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
CXCR4

警告

Toxicity: Standard Handling (A)

シーケンス

N^α-4-fluorobenzoyl-Arg-Arg-Nal-Cys⁴-Tyr-Cit-Lys-D-Lys-Pro-Tyr-Arg-Cit-Cys¹³-Arg-NH₂ (Disulfide bond: 4 → 13; Nal = L-3-(2-naphthyl)alanine; Cit = L-citrulline)

物理的形状

Supplied as a trifluoroacetate salt.

再構成

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

その他情報

Otani, Y., et al. 2012. FEBS Lett.586, 3639.
Oishi, S., and Fujii, N. 2012. Org. Biomol. Chem.10, 5720.
Tamamura, H., et al. 2003. Org. Biomol. Chem.1 3663.
Tamamura, H., et al. 2003. Org. Biomol. Chem.1, 3656.

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 1
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable