DPC-681 (DPH-153893) (Synonyms: DPH-153893) |
Catalog No.GC33968
One-Click Copy Product Info
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DPC-681(DPH-153893)은 4~40nM의 야생형 HIV-1에 대한 IC90이 있는 HIV 프로테아제의 강력하고 선택적인 억제제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 284661-68-3
Sample solution is provided at 25 µL, 10mM.
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DPC-681 is a potent and selective inhibitor of HIV protease with IC90s for wild-type HIV-1 of 4 to 40 nM.IC50 value: 4 - 40 nM [1]Target: HIV proteasein vitro: DPC 681 is extremely potent inhibitor of wild-type HIV-1. When all of the HIV-1 strains tested are considered, the average concentrations required for 90% inhibition of replication were 7.3 ± 3.4 for DPC 681. DPC 681 shows no loss in potency toward recombinant mutant HIVs with the D30N mutation and a fivefold or smaller loss in potency toward mutant variants with three to five amino acid substitutions. [1]in vivo: The total body clearance (CL) of DPC 681 in dogs was high (1.8 liter/h/kg) equaling hepatic blood flow for this species (1.8 liter/h/kg). After an oral dosing, the Cmax increased ninefold between the 10- and 30-mg/kg DPC 681 dose groups. Bioavailability also increased between the 10- and 30-mg/kg dose groups (18.3 and 78.1%, respectively). These data suggest that hepatic extraction (first-pass effect) can be saturated in the dog. [1]
[1]. Kaltenbach RF 3rd, et al. DPC 681 and DPC 684: potent, selective inhibitors of human immunodeficiency virus protease active against clinically relevant mutant variants. Antimicrob Agents Chemother. 2001 Nov;45(11):3021-8.
| Cas No. | 284661-68-3 | SDF | |
| Synonyms | DPH-153893 | ||
| Canonical 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 | ||
| Formula | C35H48FN5O5S | M.Wt | 669.85 |
| Solubility | DMSO : 100 mg/mL (149.29 mM; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.4929 mL | 7.4644 mL | 14.9287 mL |
| 5 mM | 298.6 μL | 1.4929 mL | 2.9857 mL |
| 10 mM | 149.3 μL | 746.4 μL | 1.4929 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 33 reference(s) in Google Scholar.)