| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| Other Sizes |
|
Adaptavir (DAPTA; RAP-101; mDAPTA) is a novel and potent peptide-based CCR5 receptor antagonist with the potential for the treatment of HIV infection and HBV infection.
| ln Vitro |
In monocytes/macrophages (M/M), DAPTA (1 nM) reduces HIV-1 multiplication by more than 90%. DAPTA inhibits the entrance of HIV and stops HIV-1 infection. DAPTA decreases human primary macrophage CCR5 mAb binding. Neuronal apoptosis induced by R5 gp120 is potently blocked by DAPTA. When it comes to stopping neuronal apoptosis, DAPTA is even more effective than TAK-779, a CCR5 antagonist[1]. Specific CD4-dependent binding of gp120 Bal (IC50 = 0.06 nM) and CM235 (IC50 = 0.32 nM) to CCR5 is potently inhibited by DAPTA. The formation of the gp120/sCD4 complex with CCR5 is inhibited by DAPTA (1 nM). With an IC50 of 55 ± 0.08 pM, DAPTA blocks the binding of gp120BaL/sCD4 to CCR5 (Cf2Th/synR5) cells[2].
|
|
|---|---|---|
| Enzyme Assay |
|
|
| References |
[1]. Pollicita M, et al. Profound anti-HIV-1 activity of DAPTA in monocytes/macrophages and inhibition of CCR5-mediated apoptosis in neuronal cells. Antivir Chem Chemother. 2007;18(5):285-95.
[2]. Polianova MT, et al. Chemokine receptor-5 (CCR5) is a receptor for the HIV entry inhibitor peptide T (DAPTA). Antiviral Res. 2005 Aug;67(2):83-92 |
| Molecular Formula |
C35H56N10O15
|
|---|---|
| Molecular Weight |
856.888
|
| Exact Mass |
856.3927
|
| CAS # |
106362-34-9
|
| SMILES |
C[C@@H](O)[C@@H](C(N)=O)NC([C@H](CC1=CC=C(O)C=C1)NC([C@H](CC(N)=O)NC([C@H]([C@H](O)C)NC([C@H]([C@H](O)C)NC([C@H]([C@H](O)C)NC([C@H](CO)NC([C@@H](C)N)=O)=O)=O)=O)=O)=O)=O
|
| InChi Key |
AKWRNBWMGFUAMF-ZESMOPTKSA-N
|
| InChi Code |
InChI=1S/C35H56N10O15/c1-13(36)29(54)41-22(12-46)32(57)43-26(16(4)49)34(59)45-27(17(5)50)35(60)44-25(15(3)48)33(58)40-21(11-23(37)52)30(55)39-20(10-18-6-8-19(51)9-7-18)31(56)42-24(14(2)47)28(38)53/h6-9,13-17,20-22,24-27,46-51H,10-12,36H2,1-5H3,(H2,37,52)(H2,38,53)(H,39,55)(H,40,58)(H,41,54)(H,42,56)(H,43,57)(H,44,60)(H,45,59)/t13-,14-,15-,16-,17-,20+,21+,22+,24+,25+,26+,27+/m1/s1
|
| Chemical Name |
L-Threoninamide, D-alanyl-L-seryl-L-threonyl-L-threonyl-L-threonyl-L-asparaginyl-L-tyrosyl-
|
| Synonyms |
RAP-101DAPTA mDAPTAAdaptavir D-Ala-1-peptide T-NH-2 Monomeric (D-Alanine-1) Peptide T amide
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
H2O : ~50 mg/mL (~58.35 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 10 mg/mL (11.67 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1670 mL | 5.8351 mL | 11.6701 mL | |
| 5 mM | 0.2334 mL | 1.1670 mL | 2.3340 mL | |
| 10 mM | 0.1167 mL | 0.5835 mL | 1.1670 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00951743 | Unknown † | Drug: Adaptavir (monomeric DAPTA) | HIV Infections | Rapid Laboratories Inc. | July 2009 | Phase 2 |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
