1. Anti-infection Cell Cycle/DNA Damage
  2. HIV Reverse Transcriptase DNA/RNA Synthesis Bacterial
  3. Soulattrolide

Soulattrolide 是一种具有口服效力的非核苷类 HIV-1 逆转录酶 (RT) 抑制剂,同时具备镇痛、抗炎、镇静、抗焦虑及抗菌活性;其针对 HIV-1 RT 的 IC50 值为 0.34-0.73 µM,针对 E. coli RNase HIC50 值为 69.5 µM,针对人源 DNA 聚合酶 β 的 IC50 值 >495 µM。Soulattrolide 可抑制 HIV-1 RT 的 DNA 依赖型和 RNA 依赖型 DNA 聚合酶活性、E. coli RNase H 活性,以及 Mycobacterium tuberculosis 的生长。Soulattrolide 对 HIV-2 RTAMV RT、RNA 聚合酶或 HIV-1 RTTyr181 均无活性,且不具备抗抑郁活性。Soulattrolide 可用于 HIV-1 感染、疼痛、炎症及结核分岐杆菌感染相关研究。

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Soulattrolide

Soulattrolide Chemical Structure

CAS No. : 65025-62-9

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Soulattrolide is a non-nucleoside HIV-1 reverse transcriptase (RT) inhibitor, antinociceptive, anti-inflammatory, sedative, anxiolytic, and antimicrobial agent with oral effectiveness, IC50 values of 0.34 µM for HIV-1 RT, 69.5 µM for E. coli RNase H, and >495 µM for human DNA polymerase β.Soulattrolide inhibits HIV-1 RT’s DNA-dependent and RNA-dependent DNA polymerase activities, E. coli RNase H activity, and Mycobacterium tuberculosis growth.Soulattrolide shows no activity against HIV-2 RT, AMV RT, RNA polymerase, or HIV-1 RTTyr181, and lacks antidepressant activity.Soulattrolide can be used for the research of HIV-1 infection, pain, inflammation, and Mycobacterium tuberculosis infection[1][2].

IC50 & Target[1]

HIV-1

0.34 μM (IC50)

DNA Polymerase

>495 μM (IC50)

体外研究
(In Vitro)

Soulattrolide (1.0 nM-500 μM;1 小时) 可强效抑制纯化的二聚体 HIV-1 (p66/p51) 逆转录酶的 RNA 依赖性 DNA 聚合酶活性,其 IC50 为 0.34 µM[1]
Soulattrolide (1.0 nM-500 μM;1 小时) 可抑制纯化的二聚体 HIV-1 (p66/p51) 逆转录酶的 DNA 依赖性 DNA 聚合酶活性,其 IC50 为 0.73 µM[1]
Soulattrolide (1.0 nM-500 μM;30 分钟) 可抑制纯化的大肠杆菌核糖核酸酶 H 的活性,其 IC50 为 69.5 µM[1]
Soulattrolide (495 µM;1 小时) 在最高达 495 µM 的浓度下,对 HIV-2 RT、耐 TIBO (Tyr181) 的 HIV-1 RT、禽成髓细胞瘤病毒 RT、人 DNA 聚合酶 α、人 DNA 聚合酶 β 或 Escherichia coli RNA 聚合酶均无显著抑制活性[1]
Soulattrolide (0.34 μM) 在无细胞生化实验中可强效抑制 HIV-1 逆转录酶,其 IC50 为 0.34 μM[2]
Soulattrolide (3.13 μg/mL) 在无细胞/生化实验中可抑制结核分枝杆菌的生长,其 MIC 为 3.13 μg/mL[2]

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

体内研究
(In Vivo)

Soulattrolide (0.1-50 mg/kg;口服;单次给药) 在醋酸 (10 mL/kg) 诱导的小鼠扭体模型中表现出剂量依赖性镇痛活性,其口服 ED50 为 33 mg/kg[2]
Soulattrolide (0.1-50 mg/kg;口服;单次给药) 在福尔马林 (30 μL) 诱导的小鼠舔爪模型的神经源性 (ED50 = 7 mg/kg p.o.) 和炎症性 (ED50 = 22 mg/kg p.o.) 两个阶段均表现出镇痛活性[2]
Soulattrolide (0.1-50 mg/kg;口服;单次给药) 在给药后 120 分钟进行评估时,在小鼠热板热痛觉模型中可诱导 40%的镇痛作用[2]
Soulattrolide (0.1-10 μmol/ear;局部给药;单次给药) 在 TPA (0.25 μg/μL) 诱导的小鼠耳水肿模型中呈现剂量依赖性抗炎活性,其 IC50 为 1.81 μmol/ear,且在 1 μmol/ear 剂量下可抑制 87% 的 MPO 活性[2]
Soulattrolide (1-50 mg/kg;口服;单次给药) 在戊巴比妥诱导的小鼠睡眠时间模型中发挥镇静作用,可使入睡潜伏期缩短最高达 39%,使睡眠时间延长最高达 49%[2]
Soulattrolide (1-50 mg/kg;口服;单次给药) 在小鼠转棒模型中,10 和 50 mg/kg 剂量下会损害运动协调性,该作用为一过性,于给药开始后 60 分钟消退[2]
Soulattrolide (1-50 mg/kg;口服;单次给药) 在小鼠悬尾实验中无抗抑郁活性[2]
Soulattrolide (1-50 mg/kg;口服;单次给药) 在明暗箱试验中表现出类抗焦虑作用,可显著增加小鼠在明箱区域的停留时间[2]
Soulattrolide (1-50 mg/kg;口服;单次给药) 于旷场试验中表现出类抗焦虑作用,呈剂量依赖性增加小鼠在中央区域的穿行距离[2]

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

Animal Model: Balb/c, CD-1 (male, 25-30 g)[2]
Dosage: 0.1 mg/kg; 1 mg/kg; 10 mg/kg; 50 mg/kg
Administration: p.o.; single dose
Result: Showed dose-dependent antinociceptive effects with an ED50 = 33 mg/kg.\nShowed antinociceptive activity in both phases of the formalin test, with an ED50 = 7 mg/kg for Phase 1 and an ED50 = 22 mg/kg for Phase 2.\nInduced 40% antinociception compared to the vehicle group 120 minutes post-treatment at the highest dose of 50 mg/kg.
Animal Model: Balb/c, CD-1 (male, 25-30 g)[2]
Dosage: 0.1 μmol/ear; 1 μmol/ear; 10 μmol/ear
Administration: topical; single dose
Result: Showed dose-dependent anti-inflammatory activity with an IC50 = 1.81 μmol/ear in the TPA edema test.
Inhibited MPO activity by 87% at 1 μmol/ear.
Animal Model: Balb/c, CD-1 (male, 25-30 g)[2]
Dosage: 1 mg/kg; 10 mg/kg; 50 mg/kg
Administration: p.o.; single dose
Result: Significantly decreased sleep onset by 21% (1 mg/kg), 19% (10 mg/kg), and 39% (50 mg/kg) compared to the vehicle group.
Significantly increased sleep duration by 42% (1 mg/kg), 46% (10 mg/kg), and 49% (50 mg/kg) compared to the vehicle group.\nSignificantly decreased time spent on the rotarod by 12% (10 mg/kg) and 22% (50 mg/kg) at 30 minutes post-treatment initiation.
Allowed mice to recover motor coordination by 60 minutes post-treatment initiation.\nDid not affect immobility time compared to the vehicle group.\nSignificantly increased time spent in the light compartment compared to the vehicle group, with effects similar to clonazepam (1.5 mg/kg), though not dose-dependent.\nSignificantly increased distance crossed in central squares in a dose-dependent manner, with effects similar to clonazepam (1.5 mg/kg).
分子量

404.46

Formula

C25H24O5

CAS 号
结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献
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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.

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Soulattrolide
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HY-182552
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