2. Anti-infection Cell Cycle/DNA Damage
  3. HSV DNA/RNA Synthesis
  4. (Rac)-Adibelivir

(Rac)-Adibelivir ((Rac)-IM-250) 是一种可穿透血脑屏障的 HSV 解旋酶-引物酶抑制剂与代谢稳定剂，具有抗病毒活性。(Rac)-Adibelivir 对 Acyclovir (HY-17422) 耐药株同样有效，其氘代结构具有更强的代谢稳定性，减少了羟基化代谢产物的生成。(Rac)-Adibelivir 延长了体内半衰期、降低了给药剂量、提高了口服生物利用度，并在小鼠体内实现更高的脑暴露量。(Rac)-Adibelivir 可用于单纯疱疹感染、疱疹性脑炎及阿尔茨海默病的研究。

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(Rac)-Adibelivir

(Rac)-Adibelivir Chemical Structure

CAS No. : 2137928-83-5

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规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

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Other Forms of (Rac)-Adibelivir:

(Rac)-Adibelivir 相关抗体

Top Publications Citing Use of Products

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RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

(Rac)-Adibelivir ((Rac)-IM-250) is a blood-brain barrier-penetrant HSV helicase-primase inhibitor and metabolic stabilizer with antiviral activity. (Rac)-Adibelivir is also effective against Acyclovir (HY-17422)-resistant strains, and its deuterated structure exhibits enhanced metabolic stability, reducing the formation of hydroxylated metabolites. (Rac)-Adibelivir prolongs in vivo half-life, reduces administration dosage, improves oral bioavailability, and achieves higher brain exposure in mice. (Rac)-Adibelivir can be used in the research of herpes simplex infection, herpes encephalitis and Alzheimer's disease[1].

IC50 & Target

Helicase

 

体外研究
(In Vitro)

(Rac)-Adibelivir (Example 7) 可抑制 Vero 细胞中野生型 HSV-1、HSV-2 以及耐 ACV 的 HSV-1 的复制[1]。

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

(Rac)-Adibelivir 相关抗体:

Cell Viability Assay[1]

Cell Line: Vero cells
Concentration: IC50
Incubation Time: /
Result: Inhibited wild-type HSV-1, HSV-2, and ACV-resistant HSV-1 replication in Vero cells with IC50 values of 25-100 nM, 25-100 nM, and 25-100 nM, respectively.
体内研究
(In Vivo)

(Rac)-Adibelivir (Example C7) (2-10 mg/kg；口服、静脉注射；单次) 的对映体 Example 4/2 在雄性 C57Bl/6N 小鼠中表现出 201% 的口服生物利用度和 188 mL/(h*kg) 的全身清除率[1]。
(Rac)-Adibelivir (10 mg/kg；口服；单次给药) 对映体 Example 4/2 在小鼠口服给药后，脑血浆比值达 1.57，相较于其非氘代匹配物，血浆和脑部暴露量均有所提升[1]。

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

Animal Model: C57Bl/6N Mice (male, 21-25 g)[1]
Dosage: 10 mg/kg (oral); 2 mg/kg (intravenous)
Administration: p.o.; single dose; i.v.; single dose
Result: Reached mean Cmax of 4607 ng/mL, mean AUC(0-tz) of 80231 ng*h/mL, and mean bioavailability of 201% after oral administration.
Reached mean C0 of 16.2 ng/mL, mean AUC(0-tz) of 7997 ng*h/mL, mean AUC(0-inf) of 10648 ng*h/mL, mean elimination half-life (t1/2z) of 11.3 h, mean clearance (CL) of 188 mL/(h*kg), and mean volume of distribution (Vz) of 3074 mL/kg after intravenous administration.
Animal Model: C57Bl/6N Mice (21-26 g)[1]
Dosage: 10 mg/kg
Administration: p.o.; single dose
Result: Achieved mean plasma concentration of 5474 ng/mL, mean brain concentration of 8609 ng/mL, and brain-to-plasma ratio of 1.57 at 4 hours post-dose.
分子量

435.51

Formula

C20H19F2N3O2S2
CAS 号
性状

粉末

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料
参考文献

(Rac)-Adibelivir 相关分类

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  • 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:

(Rac)-Adibelivir2137928-83-5(Rac)-IM-250HSVDNA/RNA SynthesisHerpes simplex virusherpes simplex infectionsherpesviral helicase primasehydroxylated metaboliteherpes encephalitisHSV-1miceHSV-2herpes simplex virusesAlzheimer diseaseacyclovir-resistant strainsInhibitorinhibitorinhibit

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目录号：
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