Successful, we will reply to you quickly.OK
Please select the quantity.OK
Your message is being sent, please wait.Close
Send mail failed, please send again!Close
Products are for research use only. Not for human use. We do not sell to patients.
(AMD3465 hexahydrobromide; AMD-3465 hexahydrobromide; GENZ644494 hexahydrobromide; GENZ-644494 hexahydrobromide; GENZ 644494 hexahydrobromide)
AMD 3465 hexahydrobromide Chemical Structure
|Product name: AMD 3465 hexahydrobromide|
|Cat. No.: HY-15971|
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).
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cell entry in that one of the four-nitrogen cyclam rings of the symmetrical, prototype bicyclam antagonist AMD3100 has been replaced by a two-nitrogen N-pyridinylmethylene moiety . 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 .
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 .
|M.Wt||896.07||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
H2O: ≥ 38 mg/mL
((plusmn))-BI-D is a potent ALLINI(An allosteric IN inhibitor) that binds integrase at the LEDGF/p75 binding site.
AMG 487 is a small molecule antagonist of the chemokine receptor CXCR3; inhibits binding of 125I-IP-10 and 125I-ITAC to CXCR3 (IC50 values are 8.0 and 8.2 nM respectively).
Amprenavir (Agenerase) is a HIV protease inhibitor(Ki=0.6 nM) used to treat HIV infection.
Baohuoside I (Icariside-II) is a component of Epimedium koreanum; a regulator of CXCR4 expression as well as function in cervical cancer and breast cancer cells; Apoptosis inducer.
Bevirimat(YK FH312; FH11327; MPC-4326) is an anti-HIV drug derived from a betulinic acid-like compound; is believed to inhibit HIV by a novel mechanism, so-called maturation inhibition.
BI 224436 is a novel HIV-1 non-catalytic-site integrase inhibitor; has antiviral EC50s of <15 nM against different HIV-1 laboratory strains and cellular cytotoxicity of >90 (mu)M.
BMS-806 (BMS 378806) is a small molecule gp120/CD4 inhibitor with an IC50 of median 5 nM.
BMS-538203 is a highly efficient HIV integrase inhibitor and antiviral agent.
BMS-707035 is an HIV-1 integrase (IN) inhibitor with an IC50 value of 15 nM.
CDK9-IN-1 is a novel, selective CDK9 inhibitor for the treatment of HIV infection.