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Apricitabine

Product Name
Apricitabine
CAS No.
160707-69-7
Chemical Name
Apricitabine
Synonyms
Avx754;CS-1026;Avx 754;Spd 754;(-)-dOTC;Bch 10618;APRICITABINE;(-)-Bch 10652;Unii-K1yx059ml1;Apricitabine [(-)-BCH10652
CBNumber
CB41092857
Molecular Formula
C8H11N3O3S
Formula Weight
229.26
MOL File
160707-69-7.mol
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Apricitabine Property

Boiling point:
475.4±55.0 °C(Predicted)
Density 
1.73
solubility 
DMSO: soluble
form 
A solid
pka
13.83±0.10(Predicted)
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

TRC
Product number
D245513
Product name
(-)-2''-Deoxy-3''-oxa-4''-thiocytidine(Apricitabine)
Packaging
5mg
Price
$45
Updated
2021/12/16
TRC
Product number
D245513
Product name
(-)-2''-Deoxy-3''-oxa-4''-thiocytidine(Apricitabine)
Packaging
10mg
Price
$60
Updated
2021/12/16
American Custom Chemicals Corporation
Product number
API0007304
Product name
APRICITABINE
Purity
95.00%
Packaging
1MG
Price
$157.5
Updated
2021/12/16
American Custom Chemicals Corporation
Product number
API0007304
Product name
APRICITABINE
Purity
95.00%
Packaging
5MG
Price
$501.23
Updated
2021/12/16
Biorbyt Ltd
Product number
orb180860
Product name
Apricitabine
Purity
>98%
Packaging
100mg
Price
$765
Updated
2021/12/16
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Apricitabine Chemical Properties,Usage,Production

Description

Apricitabine (formerly known as BCH-10618, SPD754, and AVX754) is a deoxycytidine nucleoside reverse transcriptase inhibitor (NRTI) in clinical development for the treatment of HIV disease. Specifically, apricitabine is the (–)-enantiomer of the heterosubstituted analog 2udeoxy-3u-oxa-4u-thiocytidine and has the molecular formula C8H11N3O3S. Apricitabine is structurally similar to lamivudine, but differs in the inversion of the oxygen and sulfur in the furanosyl ring. Apricitabine has a molecular weight of 229.26 (1 mM = 0.229 mg/ml).

Description

In common with other NRTIs, apricitabine is activated by intra-cellular phosphorylation. The initial phosphorylation to apricitabine monophosphate is catalyzed by deoxycytidine kinase. After further phosphorylation, the triphosphate form of the molecule competes with endogenous deoxycytidine triphosphate for binding to HIV-1 reverse transcriptase. The subsequent incorporation of apricitabine triphosphate into nascent DNA by this enzyme interrupts viral replication by terminating the elongation of the DNA chain. Apricitabine triphosphate is a potent and highly selective inhibitor of HIV-1 reverse transcriptase in vitro. Its inhibitory constant (Ki) for reverse transcriptase from wild-type HIV-1 (0.08 mM) was half that of lamivudine triphosphate under the same conditions and 150- to 3750- fold lower than for human DNA polymerases, including the mitochondrial DNA polymerase γ .

Uses

(-)-2''-Deoxy-3''-oxa-4''-thiocytidine (Apricitabine) is a drug that is used in the treatment of HIV aids. It as also been shown to be useful against lamivudine and zidovudine resistant virus strains

Clinical Use

Apricitabine is an NRTI currently under clinical development that has a good safety profile, including a good mitochondrial toxicity profile. There may be a niche for apricitabine in the treatment of individuals infected with viral strains with reduced susceptibility to other nucleoside analogs, including strains with M184V and TAMs. NRTIs are recommended for clinical use in combination with other classes of antiretrovirals within highly active antiretroviral treatment (HAART) regimens for HIV infection. In light of its activity in vitro against HIV strains resistant to existing NRTIs, apricitabine is likely to be most useful for the treatment of antiretroviral-experienced patients failing therapy containing one of these agents. Investigating the efficacy, tolerability, and resistance selection properties of new antiretrovirals within combination HAART regimens is complicated by the confounding effects of the other prescribed agents. Therefore, developmental NRTIs are commonly evaluated first within short-term (r14 day) trials of monotherapy in antiretroviral naive HIV-infected patients. To date, apricitabine has shown efficacy in two phase II trials, one as monotherapy in antiretroviral-naive patients, and one within HAART for antiretroviral-experienced patients.

in vivo

Apricitabine (SPD754; AVX754) (oral adminstation; 10 mg/kg; once a day) exhibits a good oral bioavailability of 68% for males and 69.4% for females rats. And the T1/2, AUC0–∞, Tmax, Cmax are 62.2 mins, 157.4 μg/min/ml and 37.3 mins, 1.16 μg/ml in female rats[1]. Apricitabine (SPD754; AVX754) (intravenous?injection; 10 mg/kg; once a day) exhibits the T1/2, AUC0–∞ values of 12.7 mins, 226.9 μg/min/ml in female rats[1].

IC 50

HIV-1

Apricitabine Preparation Products And Raw materials

Raw materials

Preparation Products

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Apricitabine Suppliers

China 33 India 1 United States 11 Global 45
Chembest Research Laboratories Limited
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160707-69-7, ApricitabineRelated Search:

Tris(hydroxymethyl)nitromethane Tris(hydroxymethyl)aminomethane Aripiprazole Olanzapine Glycine ALTRENOGEST 5-Aza-2'-deoxycytidine Gemcitabine Capecitabine 1,4-Dioxane 6-Aminocaproic acid AMINO ACIDS Apricitabine

  • APRICITABINE
  • 4-Amino-1-[(2R,4R)-2-(hydroxymethyl)-1,3-oxathiolan-4-yl]-2(1H)-pyrimidinone
  • 4-Amino-1-((2R,4R)-2-(hydroxymethyl)-1,3-oxathiolan-4-yl)pyrimidin-2(1H)-one
  • CS-1026
  • (-)-Bch 10652
  • 2(1H)-Pyrimidinone, 4-amino-1-((2R,4R)-2-(hydroxymethyl)-1,3-oxathiolan-4-yl)-
  • 2(1H)-Pyrimidinone, 4-amino-1-(2-(hydroxymethyl)-1,3-oxathiolan-4-yl)-, (2R-cis)-
  • Avx 754
  • Avx754
  • Bch 10618
  • Spd 754
  • Unii-K1yx059ml1
  • (-)-2'-Deoxy-3'-oxa-4'-thiocytidine (Apricitabine)
  • Apricitabine (AVX754, SPD754)
  • (-)-dOTC
  • Apricitabine [(-)-BCH10652
  • (-)-2'-Deoxy-3'-oxa-4'-thiocytidine
  • Apricitabine, 10 mM in DMSO
  • 160707-69-7