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Cat. No.: HY-114957

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CI-1029

CI-1029 is a HIV-1 protease inhibitor with a human IC₅₀ of 0.11 nM. CI-1029 inhibits both wild-type and mutant HIV proteases, and exhibits antiviral activity against HIV and multiple drug-resistant HIV strains, with an EC₅₀ of 6.31 μM in the presence of 30% human serum. CI-1029 can be used in studies related to HIV infection and acquired immunodeficiency syndrome (AIDS).

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

CAS No.: 207736-05-8
Formula: C₂₈H₃₇NO₄S
Molecular Weight:483.66

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

CI-1029 Chemical Structure

CAS No.: 207736-05-8

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

HIV-1 Protease

0.11 nM (IC₅₀)

In Vitro

CI-1029 (60 min) potently inhibits purified HIV-1 protease with an IC₅₀ of 0.11 nM and a K_i of 0.11 nM^[1].
CI-1029 protects HIV-IIIB-infected CEM cells with an EC₅₀ of 0.20 μM and has low cytotoxicity in uninfected CEM cells with a TC₅₀ of 210 μM, yielding a therapeutic index of 1000^[1].
CI-1029 protects HIV-infected cells in the presence of 30% human serum with an EC₅₀ of 6.31 μM^[1].
CI-1029 retains potent activity against multiple protease-resistant HIV strains in PBMCs, with a fold increase in EC₅₀ of ≤2 compared to wild-type virus^[1].

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

Parmacokinetics

Species	Dose	Route	C_max	T_1/2	AUC	Bioavailability	T_max
Mice^[1]	25 mg/kg	p.o.	26.5 μM	2.2 h	82000 nM·h/mL	/	0.5 h
Rat^[1]	10 mg/kg	p.o.	7.2	3.7 h	11.4 μg·h/mL	/	0.5 h
Dog^[1]	10 mg/kg	p.o.	77 μg/mL	1.2 h	113 μg·h/mL	33 %	/

Chemical Information

CAS No. 207736-05-8
Molecular Weight 483.66
Formula C₂₈H₃₇NO₄S
SMILES

NC(C=C1)=CC=C1CC[C@]2(CC(O)=C(C(O2)=O)SC3=C(C=C(C(C)=C3)CO)C(C)(C)C)C(C)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Hagen SE, et al. 4-Hydroxy-5,6-dihydropyrones as inhibitors of HIV protease: the effect of heterocyclic substituents at C-6 on antiviral potency and pharmacokinetic parameters. Journal of medicinal chemistry. 2001 Jul 05;44(14):2319-32. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

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100 mg

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