2. Anti-infection Metabolic Enzyme/Protease
  3. HIV Protease HIV Cytochrome P450
  4. DPC-681

DPC-681 (DPH-153893) is an orally active HIV inhibitor. DPC-681 inhibits HIV protease activity and inhibits wild-type and mutant HIV replication. DPC-681 can be used for the research of HIV infection.

For research use only. We do not sell to patients.

DPC-681

DPC-681 Chemical Structure

CAS No. : 284661-68-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO In-stock
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DPC-681 Related Antibodies

Top Publications Citing Use of Products

View All HIV Isoform Specific Products:

View All Isoforms
HIV HIV-1 HIV-2

View All Cytochrome P450 Isoform Specific Products:

View All Isoforms
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A CYP3A4 CYP17A1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

DPC-681 (DPH-153893) is an orally active HIV inhibitor. DPC-681 inhibits HIV protease activity and inhibits wild-type and mutant HIV replication. DPC-681 can be used for the research of HIV infection[1][2].

IC50 & Target[1]

HIV-1

 

CYP3A

 

In Vitro

DPC-681 (2-20 μM; 3 days) induces CYP3A4 protein expression in primary human hepatocytes in a concentration-dependent manner[1].
DPC-681 (2-20 μM; 3 days) does not significantly induce measurable CYP3A4 testosterone 6β-hydroxylase activity in primary human hepatocytes[1].
DPC-681 (2-20 μM; 3 days) induces CYP3A testosterone 6β-hydroxylase activity approximately 3-fold over vehicle control in primary male and female Sprague-Dawley rat hepatocytes[1].
DPC-681 (0.002-12.5 μM; 10 min) potently inhibits human CYP3A4-mediated testosterone 6β-hydroxylation in pooled human liver microsomes with an IC50 of 0.039 μM[1].
DPC-681 (0.002-12.5 μM; 10 min) inhibits rat CYP3A-mediated testosterone 6β-hydroxylation in pooled Sprague-Dawley rat liver microsomes with an IC50 of 1.62 μM, which is 40-fold less potent than its inhibition of human CYP3A4[1].
DPC-681 potently inhibits wild-type HIV-1 protease with a mean Ki value of 0.012 nM[2].
DPC-681 is highly selective for HIV-1 protease, with less than 50% inhibition of tested cellular proteases at concentrations of ≥13 μM[2].
DPC-681 (3-7 days) potently inhibits replication of wild-type HIV-1 strains, non-clade B isolates, and HIV-2 in MT-2, MT-4, and PBMC, with a mean IC90 of 7.3 nM across all HIV-1 strains tested[2].
DPC-681 maintains potent activity against recombinant mutant HIV-1 variants in MT-2 cells, with no loss of potency against the D30N mutant[2].
DPC-681 potently inhibits replication of 30 PI-resistant clinical HIV-1 isolates, with a mean IC50 of 18 nM and a median IC50 of 11 nM[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

DPC-681 Related Antibodies

Western Blot Analysis[1]

Cell Line: primary human hepatocytes (donors HL-N072, HL-N075, H152)
Concentration: 2; 10; 20 μM
Incubation Time: 3 days
Result: Induced CYP3A4 protein expression in a dose-dependent manner.
Parmacokinetics
Species Dose Route T1/2 CL Cmax F
Dog[2] 10 mg/kg p.o. 1.0 h / 0.9 μM 18.3 %
Dog[2] 1 mg/kg i.v. 1.0 h 1.8 / /
Dog[2] 30 mg/kg p.o. 1.7 h / 8.5 μM 78.1 %
Dog[2] 100 mg/kg p.o. 1.2 h / 22.4 μM 91.0 %
In Vivo

DPC-681 (100 mg/kg; p.o.; twice daily, 6 hours apart; 12 days) autoinduces its own metabolism in Sprague-Dawley rats, increasing hepatic CYP3A activity 4-fold in males and 21-fold in females after 12 days of twice-daily 100 mg/kg oral dosing[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague-Dawley rats (12-week-old male and female, 250-300 g)[1]
Dosage: 100 mg/kg
Administration: p.o.; twice daily, 6 hours apart; 12 days
Result: Reduced AUC0-6ₕ to less than 20% of day 1 values in male and female rats.
Induced hepatic CYP3A activity 4-fold in male rats and 21-fold in female rats relative to vehicle controls.
Molecular Weight

669.85

Formula

C35H48FN5O5S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=S(C1=CC(N)=CC=C1)(N(C[C@@H](O)[C@H](CC2=CC=CC=C2)NC([C@H](C(C)(C)C)NC(CNCC3=CC=CC(F)=C3)=O)=O)CC(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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (149.29 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 1.4929 mL 7.4644 mL 14.9287 mL
5 mM 0.2986 mL 1.4929 mL 2.9857 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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Volume (start)

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C2

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V2

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

Dosage

mg/kg

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(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

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

Purity: 99.72%

SDS (252 KB)

COA (251 KB) LCMS (123 KB)

Handling Instructions (2659 KB)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.4929 mL 7.4644 mL 14.9287 mL 37.3218 mL
5 mM 0.2986 mL 1.4929 mL 2.9857 mL 7.4644 mL
10 mM 0.1493 mL 0.7464 mL 1.4929 mL 3.7322 mL
15 mM 0.0995 mL 0.4976 mL 0.9952 mL 2.4881 mL
20 mM 0.0746 mL 0.3732 mL 0.7464 mL 1.8661 mL
25 mM 0.0597 mL 0.2986 mL 0.5971 mL 1.4929 mL
30 mM 0.0498 mL 0.2488 mL 0.4976 mL 1.2441 mL
40 mM 0.0373 mL 0.1866 mL 0.3732 mL 0.9330 mL
50 mM 0.0299 mL 0.1493 mL 0.2986 mL 0.7464 mL
60 mM 0.0249 mL 0.1244 mL 0.2488 mL 0.6220 mL
80 mM 0.0187 mL 0.0933 mL 0.1866 mL 0.4665 mL
100 mM 0.0149 mL 0.0746 mL 0.1493 mL 0.3732 mL
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DPC-681 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:

DPC-681284661-68-3DPH-153893DPC681DPC 681DPH153893DPH 153893HIV ProteaseHIVCytochrome P450Human immunodeficiency virusCYPsMT-2 cellsHIV proteaseprimary human hepatocytespooled human liver microsomesSprague-Dawley rat hepatocytesCYP3A4rat CYP3Apooled Sprague-Dawley rat liver microsomeshuman HIV-1 proteasebeagle dogsInhibitorinhibitorinhibit

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