Pirmitegravir
Based on 1 Customer Validation
Pirmitegravir is a potent and first-in-class inhibitor of allosteric integrase (ALLINI) that targets LEDGF/p75 binding site. Pirmitegravir displays picomolar IC50 in human PBMCs with a >24,000 therapeutic index against HIV-1. Pirmitegravir harbors outstanding anti-virus and safety properties.
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- Pureté: 99.79%
- CAS No.: 2245231-10-9
- Formule: C27H31ClN4O3
- Masse moléculaire:495.01
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
allosteric integrase (ALLINI)[1]
Pirmitegravir (Compound STP0404) inhibits dual tropic HIV-189.6 at 1.4 nM IC50 in CEMx174 cells[1].
Pirmitegravir (Compound STP0404) is a highly potent ALLINI with picomolar to single-digit nanomolar IC50 values that inhibits both wild type and Ral-resistant HIV-1 strains[1].
Pirmitegravir (Compound STP0404) displays IC50 of 0.41 nM against HIV-1NL4-3 without observable cytotoxicity in human PBMCs at 10 μM (TC50 >10μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pirmitegravir (Compound STP0404) lacks micronucleus-inducing and bone marrow cell proliferation inhibitory potentials in rats (500, 1000 and 2000 mg/kg/day), supporting that STP0404 is not genotoxic[1].
Assessment of Pharmacokinetics (PK) profile of Pirmitegravir (Compound STP0404) in rat and dog[1].
| PK Values | Rat | Dog | ||
| 10 mg/kg (p.o) | 5 mg/kg (i.v) | 2 mg/kg (p.o) | 2 mg/kg (i.v) | |
| T1/2 (hr) | 4.56 | 3.83 | 6.90 | 6.11 |
| AUC (hr.nM) | 78074 | 42676 | 4683 | 9260 |
| Cmax (nM) | 21380 | - | 3983 | - |
| Ft (%) | 92.8 | - | 50.6 | - |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SD rats and beagle dogs[1]
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Dosage:1, 2, 5, and 10 mg/kg
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Administration:i.v.; p.o.
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Result:The half-life (T1/2) was 3–7 h, and oral bioavailability (Ft) was 50–93% in these two animal species. Systemic exposure, which was determined by area under the curve and maximum concentration of STP0404 in plasma (AUC and Cmax), increased dose-dependently from 2 to 10 mg/kg.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2245231-10-9
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Appearance Solid
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Masse moléculaire 495.01
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Formule C27H31ClN4O3
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Color White to off-white
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SMILES
O=C([C@H](C1=C(N=C(C2=C1C3=CC=C(C=C3)Cl)N(C(C)=C2C)CC4=CN(N=C4)C)C)OC(C)(C)C)O
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Synonyms
STP0404
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 125 mg/mL (252.52 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (277 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.0202 mL | 10.1008 mL | 20.2016 mL | 50.5040 mL |
| 5 mM | 0.4040 mL | 2.0202 mL | 4.0403 mL | 10.1008 mL | |
| 10 mM | 0.2020 mL | 1.0101 mL | 2.0202 mL | 5.0504 mL | |
| 15 mM | 0.1347 mL | 0.6734 mL | 1.3468 mL | 3.3669 mL | |
| 20 mM | 0.1010 mL | 0.5050 mL | 1.0101 mL | 2.5252 mL | |
| 25 mM | 0.0808 mL | 0.4040 mL | 0.8081 mL | 2.0202 mL | |
| 30 mM | 0.0673 mL | 0.3367 mL | 0.6734 mL | 1.6835 mL | |
| 40 mM | 0.0505 mL | 0.2525 mL | 0.5050 mL | 1.2626 mL | |
| 50 mM | 0.0404 mL | 0.2020 mL | 0.4040 mL | 1.0101 mL | |
| 60 mM | 0.0337 mL | 0.1683 mL | 0.3367 mL | 0.8417 mL | |
| 80 mM | 0.0253 mL | 0.1263 mL | 0.2525 mL | 0.6313 mL | |
| 100 mM | 0.0202 mL | 0.1010 mL | 0.2020 mL | 0.5050 mL |
Pirmitegravir Related Classifications
HY-130000 Related Classifications
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