2. Others Anti-infection Metabolic Enzyme/Protease
  3. Drug Intermediate HIV Reverse Transcriptase Carbonic Anhydrase
  4. Elsulfavirine sodium

Elsulfavirine sodium (R-1206 sodium) 是一种口服有效的人碳酸酐酶 (carbonic anhydrase，CA) 抑制剂和 HIV-1 非核苷类逆转录酶 (NNRT) 别构抑制剂。Elsulfavirine sodium 还靶向阻断腺苷酸琥珀酸裂解酶 (ADSL) 与胰岛素诱导基因蛋白 INSIG1/2 的相互作用，阻断 SREBP-1 介导的脂质从头合成，抑制肝癌细胞增殖。Elsulfavirine sodium 与 Lenvatinib (HY-10981) 联用可产生协同抗肿瘤作用。Elsulfavirine sodium 在体内可转化为活性代谢物 VM1500A，阻断逆转录酶的 DNA 聚合活性，抑制 HIV-1 复制。Elsulfavirine sodium 对人碳酸酐酶 I、VII、VI、VA、VB、IX、XIII、XIV 等亚型的 Ki=1960 nM-52400 nM。Elsulfavirine sodium 被用于 HIV-1 感染和肝癌的相关研究。

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Elsulfavirine sodium

Elsulfavirine sodium Chemical Structure

CAS No. : 867365-40-0

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Elsulfavirine sodium 的其他形式现货产品:

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Other Forms of Elsulfavirine sodium:

Elsulfavirine sodium 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 1 篇科研文献

查看 HIV 亚型特异性产品:

查看所有亚型
HIV HIV-1 HIV-2

查看 Carbonic Anhydrase 亚型特异性产品:

查看所有亚型
CA CA I CA Ⅱ CA IX CA XII CA VII CA VI CA VA CA VB CA XIII CA XIV

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Elsulfavirine sodium (R-1206 sodium) is an orally active human carbonic anhydrase (carbonic anhydrase, CA) inhibitor and an allosteric inhibitor of HIV-1 non-nucleoside reverse transcriptase (NNRT). Elsulfavirine sodium also targets and blocks the interaction between adenylosuccinate lyase (ADSL) and insulin-induced gene proteins INSIG1/2, blocks SREBP-1-mediated de novo lipid synthesis, and inhibits the proliferation of liver cancer cells. The combination of Elsulfavirine sodium and Lenvatinib (HY-10981) produces a synergistic anti-tumor effect. Elsulfavirine sodium is converted into the active metabolite VM1500A in vivo, blocks the DNA polymerase activity of reverse transcriptase, and inhibits HIV-1 replication. Elsulfavirine sodium exhibits a Ki of 1960 nM-52400 nM against human carbonic anhydrase isoforms including I, VII, VI, VA, VB, IX, XIII, XIV. Elsulfavirine sodium is used in studies related to HIV-1 infection and liver cancer[1][2][3][4].

IC50 & Target[1][2][3][4]

HIV-1

 

hCA I

52400 nM (Ki)

hCA II

12500 nM (Ki)

CA VA

4290 nM (Ki)

CA VB

14200 nM (Ki)

CA VI

5670 nM (Ki)

hCA IX

2390 nM (Ki)

hCA IX

6650 nM (Ki)

hCA XII

9801 nM (Ki)

CA XIII

4820 nM (Ki)

CA XIV

1960 nM (Ki)

体外研究
(In Vitro)

Elsulfavirine (10 μM；1 h) sodium 可显著阻断高糖诱导的 Huh7 细胞内 ADSL 与 INSIG1/2 的相互作用，抑制 SREBP-1 的剪切活化与核转位，并阻断 SRE 驱动的荧光素酶转录活性，抑制 SREBP 脂合成通路的激活[2]。
Elsulfavirine (10 μM；12 h) sodium 可显著抑制高糖诱导的 Huh7 细胞中 SCAP 从内质网向高尔基体的转运，下调 SREBP-1 下游脂合成靶基因 FASN、ACACA、SCD、GPAM 的 mRNA 表达水平，同时减少细胞内脂滴的数量，抑制高糖诱导的细胞内脂质蓄积[2]。
Elsulfavirine (10 μM；8 h) sodium 可显著抑制 Huh7 细胞中14C -葡萄糖向甘油三酯和脂肪酸的转化，阻断细胞内的新生脂质合成过程[2]。
Elsulfavirine sodium 的活性代谢产物 VM-1500A (血清校正 EC50 约 13.8 nM) 可在体外细胞模型中有效抑制 HIV-1 临床分离株的复制[3]。

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

Elsulfavirine sodium 相关抗体:

Western Blot Analysis[2]

Cell Line: Huh7 human hepatocellular carcinoma cells
Concentration: 10 μM (elsulfavirine), 20 μM (tezacaftor), 100 μM (pyrithioxin) as control compounds
Incubation Time: 1 h pre-treatment before high-glucose stimulation
Result: Markedly suppressed the cleavage and activation of SREBP-1 induced by high glucose in Huh7 cells, while it did not affect the phosphorylation of ADSL at S407 mediated by PKCε.
In contrast, the control compounds tezacaftor and pyrithioxin showed no significant inhibitory effect on SREBP-1 cleavage.

Real Time qPCR[2]

Cell Line: Huh7 human hepatocellular carcinoma cells
Concentration: 10 μM
Incubation Time: 12 h co-treatment with high glucose
Result: Significantly downregulated the high glucose-induced mRNA expression of SREBP-1 downstream lipogenic target genes, including FASN, ACACA, SCD and GPAM, in Huh7 cells.
体内研究
(In Vivo)

Elsulfavirine sodium (10 mg/kg；口服；每日 1 次；20 天) 在裸鼠 Huh7 细胞皮下异种移植肝癌模型中，显著抑制肝癌肿瘤生长，降低肿瘤组织中增殖标志物 Ki-67 的表达、提升肿瘤细胞凋亡水平，同时下调 SREBP-1 及 FASN、ACLY 的蛋白表达[2]。
Elsulfavirine sodium (10 mg/kg；口服；每日 1 次；连续给药 20 天) 联合 Lenvatinib (HY-10981) (给药方式同 Elsulfavirine) 在裸鼠 Huh7 细胞皮下异种移植肝癌模型中，协同抑制肝癌肿瘤生长，比单试剂处理的效果更好[2]。

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

Animal Model: Male athymic BALB/c nude mice (6-week-old) with subcutaneous xenograft hepatocellular carcinoma (HCC) model established by subcutaneous inoculation of 1 × 106 Huh7 cells in the right flank[2]10 mg/kg
Dosage: 10 mg/kg
Administration: Administered via gavage once daily for 20 consecutive days, starting on day 7 after tumor cell inoculation; with 10 mg/kg lenvatinib or not.
Result: As for monotherapy:
Significantly inhibited the growth of HCC xenografts in nude mice, reduced the expression of proliferation marker Ki-67 in tumor tissues, increased the level of tumor cell apoptosis, and downregulated the protein expression of SREBP-1 and lipogenesis-related enzymes including FASN and ACLY in tumor tissues, compared with the vehicle control group.
As for combination:
Exerted a synergistic inhibitory effect on HCC tumor growth, with a more significant reduction in tumor volume and weight, lower Ki-67 expression, higher tumor cell apoptosis, and more pronounced downregulation of SREBP-1, FASN and ACLY in tumor tissues, compared with the Elsulfavirine or lenvatinib monotherapy groups.
分子量

652.27

Formula

C24H17BrCl2FN3NaO5S
CAS 号
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

Elsulfavirine sodium 相关分类

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Keywords:

Elsulfavirine867365-40-0R-1206R1206R 1206Drug IntermediateHIVReverse TranscriptaseCarbonic AnhydraseDrug IintermediateHuman immunodeficiency virusCarbonate dehydratasehuman carbonic anhydrase VAhuman carbonic anhydrase Ihuman carbonic anhydrase VBhuman carbonic anhydrase VIHIV-1 infectionshuman carbonic anhydrase XIIIhuman carbonic anhydrase XIVhuman carbonic anhydrase VIIhuman carbonic anhydrase IXhuman carbonic anhydrase IIInhibitorinhibitorinhibit

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