| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| ln Vitro |
In single-cycle experiments, BMS-986001's average EC50 was 74 nM for HIV-2ROD9 and 890 nM for HIV-1NL4-3, indicating that it is more potent against HIV-2ROD9 than HIV-1NL4-3. In a 4-day infection of immortalized T cell lines (CEMss), HIV-2ROD9 also shown increased sensitivity to BMS-986001; the average EC50 of HIV-2ROD9 (EC50 of 0.14 nM) was 30-fold lower than that of HIV 1NL4-3 (EC50 of 4.2 nM) [1]. BMS-986001 demonstrates complete efficacy against HIV-2 strains that have single amino acid alterations encoded in their reverse transcriptases, K65R and Q151M [1].
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| ln Vivo |
Pharmacokinetic characteristics of sensavudine (BMS-986001; 100-750 mg/kg) derived from dried blood spot (DBS) assays and plasma assays were compared. Across all dose groups in rats, the AUC(0-24 h) and C max of BMS-986001 in DBS were consistent with the ratios in plasma, 0.83-0.91 and 0.81-0.97, respectively. The T max in rat DBS and plasma is also constant at roughly 1 hour [2].
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| References |
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| Additional Infomation |
Censavudine has been used in trials studying the treatment of HIV-1 Infection.
Drug Indication Treatment of Aicardi-Goutières syndrome |
| Molecular Formula |
C12H12N2O4
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|---|---|
| Molecular Weight |
248.2347
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| Exact Mass |
248.08
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| CAS # |
634907-30-5
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| Related CAS # |
(2S,5S)-Censavudine
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| PubChem CID |
3008897
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
-0.7
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
18
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| Complexity |
513
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| Defined Atom Stereocenter Count |
2
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| SMILES |
O1[C@](C#C[H])(C([H])([H])O[H])C([H])=C([H])[C@]1([H])N1C(N([H])C(C(C([H])([H])[H])=C1[H])=O)=O
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| InChi Key |
OSYWBJSVKUFFSU-SKDRFNHKSA-N
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| InChi Code |
InChI=1S/C12H12N2O4/c1-3-12(7-15)5-4-9(18-12)14-6-8(2)10(16)13-11(14)17/h1,4-6,9,15H,7H2,2H3,(H,13,16,17)/t9-,12+/m1/s1
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| Chemical Name |
1-[(2R,5R)-5-ethynyl-5-(hydroxymethyl)-2H-furan-2-yl]-5-methylpyrimidine-2,4-dione
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~52 mg/mL (~209.48 mM)
H2O : ~10 mg/mL (~40.29 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.83 mg/mL (11.40 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 28.3 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.83 mg/mL (11.40 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 28.3 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0285 mL | 20.1426 mL | 40.2852 mL | |
| 5 mM | 0.8057 mL | 4.0285 mL | 8.0570 mL | |
| 10 mM | 0.4029 mL | 2.0143 mL | 4.0285 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 |
| NCT05613868 | RECRUITING | Drug: TPN-101 | Aicardi-Goutières Syndrome (AGS) | Transposon Therapeutics, Inc. | 2023-03-15 | Phase 2 |
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