2. Anti-infection Cell Cycle/DNA Damage
  3. HIV Reverse Transcriptase Nucleoside Antimetabolite/Analog
  4. AzddMeC

AzddMeC (CS-92) is an antiviral nucleoside analogue and a potent potent, selective and orally active HIV-1 reverse transcriptase and HIV-1 replication inhibitor. In HIV-1-infected human PBM cells and HIV-1-infected human macrophages, the EC50 values of AzddMeC are 9 nM and 6 nM, respectively. AzddMeC is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.

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AzddMeC Chemical Structure

AzddMeC Chemical Structure

CAS No. : 87190-79-2

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Based on 1 publication(s) in Google Scholar

AzddMeC Related Antibodies

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Description

AzddMeC (CS-92) is an antiviral nucleoside analogue and a potent potent, selective and orally active HIV-1 reverse transcriptase and HIV-1 replication inhibitor. In HIV-1-infected human PBM cells and HIV-1-infected human macrophages, the EC50 values of AzddMeC are 9 nM and 6 nM, respectively[1][2]. AzddMeC is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.

IC50 & Target[1]

HIV-2

 

HIV-1

9 nM (EC50, Human PBM cells)

HIV-1

6 nM (EC50, Human macrophages)

In Vitro

AzddMeC (CS-92) is also effective against HIV-2 in lymphocytes. The replication of Friend murine virus is only weakly inhibited, and no effect is observed against HSV type 1 and type 2 and coxsackievirus B4. The interaction of the 5'-triphosphate of AzddMeC with HIV-1 reverse transcriptase indicated competitive inhibition (the inhibition constant, Kis, is 9.3 nM)[1].

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

AzddMeC Related Antibodies
In Vivo

The pharmacokinetics of AzddMeC are characterized following intravenous and oral administration of 60 mg/kg of the compound to male rhesus monkeys. 3'-azido-3'-deoxythymidine (AZT) is a major metabolite of AzddMeC in monkeys. AzddMeC concentrations in serum declined rapidly in a biexponential fashion with the terminal half-life ranging from 0.5 to 1.3 hr. Renal excretion of unchanged nucleoside and metabolic deamination yielding AZT are the primary routes of AzddMeC clearance. The oral bioavailability is 26%[2].

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

266.26

Formula

C10H14N6O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1N([C@H]2C[C@H](N=[N+]=[N-])[C@@H](CO)O2)C=C(C)C(N)=N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (751.15 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 3.7557 mL 18.7786 mL 37.5573 mL
5 mM 0.7511 mL 3.7557 mL 7.5115 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 (sealed storage, away from moisture). 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
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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 (sealed storage, away from moisture). 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 3.7557 mL 18.7786 mL 37.5573 mL 93.8932 mL
5 mM 0.7511 mL 3.7557 mL 7.5115 mL 18.7786 mL
10 mM 0.3756 mL 1.8779 mL 3.7557 mL 9.3893 mL
15 mM 0.2504 mL 1.2519 mL 2.5038 mL 6.2595 mL
20 mM 0.1878 mL 0.9389 mL 1.8779 mL 4.6947 mL
25 mM 0.1502 mL 0.7511 mL 1.5023 mL 3.7557 mL
30 mM 0.1252 mL 0.6260 mL 1.2519 mL 3.1298 mL
40 mM 0.0939 mL 0.4695 mL 0.9389 mL 2.3473 mL
50 mM 0.0751 mL 0.3756 mL 0.7511 mL 1.8779 mL
60 mM 0.0626 mL 0.3130 mL 0.6260 mL 1.5649 mL
80 mM 0.0469 mL 0.2347 mL 0.4695 mL 1.1737 mL
100 mM 0.0376 mL 0.1878 mL 0.3756 mL 0.9389 mL
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AzddMeC 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:

AzddMeC87190-79-2CS-92CS92CS 92HIVReverse TranscriptaseNucleoside Antimetabolite/AnalogHuman immunodeficiency virusHIV-1nucleosideanalogAZTantiviralreversetranscriptasereplicationHIV-2Inhibitorinhibitorinhibit

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