[CAS NO. 7481-89-2] Zalcitabine

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PRODUCTS SPECIFICATIONS [7481-89-2]

Catalog

HY-17392

Brand

MCE

CAS

7481-89-2

DESCRIPTION [7481-89-2]

Overview

MDL	MFCD00012188
Molecular Weight	211.22
Molecular Formula	C9H13N3O3
SMILES	OC[C@@H]1CC[C@H](N2C(N=C(C=C2)N)=O)O1

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

3 Publications Citing Use of MCE

Summary

Zalcitabine is a potent nucleoside analogue reverse transcriptase inhibitor used in the treatment of HIV infection .

IC50 & Target

Target: HIV

In Vitro

Zalcitabine is a dideoxynucleoside antiretroviral agent that is phosphorylated to the active metabolite 2',3'-dideoxycytidine 5'-triphosphate (ddCTP) within both uninfected and HIV-infected cells. At therapeutic concentrations, ddCTP inhibits HIV replication by inhibiting the enzyme reverse transcriptase and terminating elongation of the proviral DNA chain ^[1] . Zalcitabine exhibits the inhibition effect on the cellular uptake of [3H]-PAH in CHO/hOAT1 cells with an IC ₅₀ value of 1.23 mM. Furthermore, the cellular uptake of zalcitabine increased threefold with the enhancement of hOATI activity in CHO/hOAT1 cells ^[2] .

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

Clinical Trial

NCT Number	Sponsor	Condition	Phase
NCT00001048	National Institute of Allergy and Infectious Diseases (NIAID)\|Bristol-Myers Squibb\|Upjohn	HIV Infections\|Leukoencephalopathy, Progressive Multifocal	Phase 2
NCT00000978	National Institute of Allergy and Infectious Diseases (NIAID)\|Hoffmann-La Roche	HIV Infections	Phase 1
NCT00002162	Hoffmann-La Roche\|NIH AIDS Clinical Trials Information Service	HIV Infections	Phase 2
NCT00000704	National Institute of Allergy and Infectious Diseases (NIAID)	HIV Infections	Phase 1
NCT00001040	Hoffmann-La Roche\|National Institute of Allergy and Infectious Diseases (NIAID)	HIV Infections	Phase 2
NCT00000682	National Institute of Allergy and Infectious Diseases (NIAID)	HIV Infections	Phase 3
NCT00002265	Hoffmann-La Roche\|NIH AIDS Clinical Trials Information Service	HIV Infections	Phase 2
NCT00000653	National Institute of Allergy and Infectious Diseases (NIAID)\|Hoffmann-La Roche	HIV Infections	Phase 2
NCT00000969	National Institute of Allergy and Infectious Diseases (NIAID)\|Bristol-Myers Squibb\|Hoffmann-La Roche	HIV Infections	Not Applicable
NCT00002086	Glaxo Wellcome\|NIH AIDS Clinical Trials Information Service	HIV Infections	Phase 2
NCT00002117	Hoffmann-La Roche\|NIH AIDS Clinical Trials Information Service	HIV Infections	Phase 3
NCT00000718	National Institute of Allergy and Infectious Diseases (NIAID)\|Hoffmann-La Roche	HIV Infections	Not Applicable
NCT00002081	Hoffmann-La Roche\|NIH AIDS Clinical Trials Information Service	HIV Infections	Not Applicable
NCT00002256	Hoffmann-La Roche\|NIH AIDS Clinical Trials Information Service	HIV Infections	Not Applicable
NCT00000781	National Institute of Allergy and Infectious Diseases (NIAID)\|Bristol-Myers Squibb\|Glaxo Wellcome	HIV Infections	Phase 2
NCT00000954	National Institute of Allergy and Infectious Diseases (NIAID)\|Novum\|Bristol-Myers Squibb	Sarcoma, Kaposi\|HIV Infections	Phase 1
NCT00001035	National Institute of Allergy and Infectious Diseases (NIAID)\|Schering-Plough	HIV Infections\|Hepatitis C	Phase 1
NCT00000678	National Institute of Allergy and Infectious Diseases (NIAID)\|Hoffmann-La Roche	HIV Infections	Phase 2
NCT00000902	National Institute of Allergy and Infectious Diseases (NIAID)	HIV Infections	Phase 1
NCT00002334	Hoffmann-La Roche\|NIH AIDS Clinical Trials Information Service	HIV Infections	Phase 3
NCT00002001	Glaxo Wellcome\|NIH AIDS Clinical Trials Information Service	HIV Infections	Not Applicable
NCT00000651	National Institute of Allergy and Infectious Diseases (NIAID)\|Hoffmann-La Roche\|Glaxo Wellcome	HIV Infections	Phase 3
NCT00002386	Merck Sharp & Dohme LLC\|NIH AIDS Clinical Trials Information Service	HIV Infections\|Hemophilia A	Phase 4
NCT00002118	Hoffmann-La Roche\|NIH AIDS Clinical Trials Information Service	HIV Infections	Not Applicable
NCT00000997	National Institute of Allergy and Infectious Diseases (NIAID)	HIV Infections	Not Applicable
NCT00002109	Immunobiology Research Institute\|NIH AIDS Clinical Trials Information Service	HIV Infections	Phase 3
NCT00002279	Hoffmann-La Roche\|NIH AIDS Clinical Trials Information Service	HIV Infections	Not Applicable
NCT00001022	National Institute of Allergy and Infectious Diseases (NIAID)	HIV Infections	Phase 3
NCT00001029	National Institute of Allergy and Infectious Diseases (NIAID)\|Bristol-Myers Squibb\|Glaxo Wellcome	HIV Infections	Phase 2
NCT00001032	National Institute of Allergy and Infectious Diseases (NIAID)	HIV Infections	Phase 2
NCT00000753	National Institute of Allergy and Infectious Diseases (NIAID)\|Upjohn\|Glaxo Wellcome	HIV Infections	Phase 1
NCT00002347	Parexel\|NIH AIDS Clinical Trials Information Service	HIV Infections	Phase 2
NCT00001087	National Institute of Allergy and Infectious Diseases (NIAID)	HIV Infections	Phase 2
NCT00000679	National Institute of Allergy and Infectious Diseases (NIAID)\|Hoffmann-La Roche	HIV Infections	Phase 2
NCT00002436	Glaxo Wellcome\|NIH AIDS Clinical Trials Information Service	HIV Infections	Phase 3
NCT00000719	National Institute of Allergy and Infectious Diseases (NIAID)	HIV Infections	Not Applicable
NCT00002333	Hoffmann-La Roche\|NIH AIDS Clinical Trials Information Service	HIV Infections	Phase 2
NCT00000754	National Institute of Allergy and Infectious Diseases (NIAID)\|Hoffmann-La Roche\|Glaxo Wellcome	HIV Infections	Phase 2
NCT00000625	National Institute of Allergy and Infectious Diseases (NIAID)\|Bristol-Myers Squibb\|Glaxo Wellcome	HIV Infections	Phase 2

Appearance

Solid

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 : 62.5 mg/mL ( 295.90 mM ; Need ultrasonic)

H ₂ O : ≥ 25 mg/mL ( 118.36 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	4.7344 mL	23.6720 mL	47.3440 mL
5 mM	0.9469 mL	4.7344 mL	9.4688 mL
10 mM	0.4734 mL	2.3672 mL	4.7344 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.08 mg/mL (9.85 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (9.85 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.08 mg/mL (9.85 mM); Clear solution

* All of the co-solvents are available by MCE.

References

Synonyms

Cytidine, 2′,3′-dideoxy-

2′,3′-Dideoxycytidine

NSC 606170

ddC

Dideoxycytidine

Ro 24-2027/000

Zalcitabine

D 2C

Hivid