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AMD 3465 hexahydrobromide

HY-15971

(AMD3465 hexahydrobromide; AMD-3465 hexahydrobromide; GENZ644494 hexahydrobromide; GENZ-644494 hexahydrobromide; GENZ 644494 hexahydrobromide)

AMD 3465 hexahydrobromide

AMD 3465 hexahydrobromide Chemical Structure

AMD 3465 6HBr(GENZ-644494) is a potent, selective CXCR4 antagonist; exhibits 8-fold higher affinity than AMD 3100; inhibits SDF-1α-ligand binding (Ki = 41.7 nM).

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Free sample   Apply now  
10 mM * 1 mL in DMSO $88 In-stock
10 mg $80 In-stock
50 mg $260 In-stock
100 mg $480 In-stock
200 mg Get quote
500 mg Get quote
Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO €86 In-stock
10 mg €78 In-stock
50 mg €255 In-stock
100 mg €470 In-stock
200 mg Get quote
500 mg Get quote

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Product name: AMD 3465 hexahydrobromide
Cat. No.: HY-15971

AMD 3465 hexahydrobromide Data Sheet

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    DataSheet

Related Compound Libraries

Biological Activity of AMD 3465 hexahydrobromide

AMD 3465 6HBr(GENZ-644494) is a potent, selective CXCR4 antagonist; exhibits 8-fold higher affinity than AMD 3100; inhibits SDF-1α-ligand binding (Ki = 41.7 nM).
IC50 value:
Target: CXCR4 
in vitro: AMD3465 is a novel, nonpeptide CXCR4 antagonist and a potent inhibitor of HIV cell entry in that one of the four-nitrogen cyclam rings of the symmetrical, prototype bicyclam antagonist AMD3100 has been replaced by a two-nitrogen N-pyridinylmethylene moiety [1]. AMD3465 is an antagonist of SDF-1 ligand binding (K(i) of 41.7+/-1.2nM), and inhibits SDF-1 mediated signaling as shown by inhibition of GTP binding, calcium flux, and inhibition of chemotaxis. AMD3465 is selective for CXCR4 and does not inhibit chemokine-stimulated calcium flux in cells expressing CXCR3, CCR1, CCR2b, CCR4, CCR5 or CCR7, nor does it inhibit binding of LTB(4) to its receptor, BLT1 [2].
in vivo: The pharmacokinetics of AMD3465 was investigated in mice and dogs. Absorption was rapid following subcutaneous administration. AMD3465 was cleared from dog plasma in a biphasic manner with a terminal half-life of 1.56-4.63h. Comparison of exposure to the intravenous and subcutaneous doses indicated 100% bioavailability following subcutaneous administration. AMD3465 caused leukocytosis when administered subcutaneously in mice and dogs, with peak mobilization occurring between 0.5 and 1.5h following subcutaneous dosing in mice and with maximum peak plasma concentration of compound preceding peak mobilization in dogs, indicating that AMD3465 has the potential to mobilize hematopoietic stem cells [2].

Protocol (Extracted from published papers and Only for reference)

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Chemical Information

M.Wt 410.6 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C24H38N6
CAS No 185991-07-5
Solvent & Solubility

Soluble to 50 mM in water and to 25 mM in DMSO

Preparing Stock Solutions

1 mg 5 mg 10 mg
1 mM 2.4355 mL 12.1773 mL 24.3546 mL
5 mM 0.4871 mL 2.4355 mL 4.8709 mL
10 mM 0.2435 mL 1.2177 mL 2.4355 mL

References on AMD 3465 hexahydrobromide

Other Forms

  • AMD 3465

    CAS No.: 185991-24-6 Get quote

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