2. Metabolic Enzyme/Protease Anti-infection
  3. HIV Integrase HIV
  4. Pirmitegravir

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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Pirmitegravir Chemical Structure

Pirmitegravir Chemical Structure

CAS No. : 2245231-10-9

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Based on 1 publication(s) in Google Scholar

Pirmitegravir Related Antibodies

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Description

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[1].

IC50 & Target

allosteric integrase (ALLINI)[1]
In Vitro

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 Related Antibodies
In Vivo

Pirmitegravir (Compound STP0404) displays appropriate PK profiles for once daily administration[1].
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.

Animal Model: SD rats and beagle dogs[1]
Dosage: 1, 2, 5, and 10 mg/kg
Administration: i.v.; p.o.
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.
Clinical Trial
Molecular Weight

495.01

Formula

C27H31ClN4O3
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0202 mL 10.1008 mL 20.2016 mL
5 mM 0.4040 mL 2.0202 mL 4.0403 mL
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

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
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
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Pirmitegravir Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Pirmitegravir2245231-10-9STP0404STP 0404STP-0404HIV IntegraseHIVHuman immunodeficiency virusallosteric integraseALLINILEDGF/p75HIV-1anti-virussafetycytotoxicityInhibitorinhibitorinhibit

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