5.00507
CXCR4 Antagonist IV, TF14016
别名:
CXCR4 Antagonist IV, TF14016, Fusin Antagonist IV
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关于此项目
经验公式（希尔记法）:
C101H145FN34O18S2 · xH2O
分子量:
2206.58 (anhydrous basis)
NACRES:
NA.77
UNSPSC Code:
51111800
Assay:
≥95% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
assay
≥95% (HPLC)
Quality Segment
form
solid
potency
0.9 nM IC50
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
white
solubility
H2O: 100 mg/mL
storage temp.
−20°C
General description
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-1IIIB 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.
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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
CXCR4
CXCR4
Physical form
Supplied as a trifluoroacetate salt.
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Nα-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)
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.
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
怎么回事？
WGK 1
闪点 (F)
Not applicable
闪点 (°C)
Not applicable