1. Others Metabolic Enzyme/Protease Cytoskeleton Cell Cycle/DNA Damage
  2. Drug Derivative NAMPT Microtubule/Tubulin
  3. Carba1

Carba1 是一种双功能 Carbazole (HY-D0204) 衍生物,能激活烟酰胺磷酸核糖转酶 (NAMPT) 并增强 NAD 的生物合成。Carba1 与微管蛋白 (tubulin) 的秋水仙碱结合位点结合,可增强多种化疗药物的抗肿瘤效果,如 Paclitaxel (HY-B0015)。Carba1 具有神经保护作用,还能调节细胞能量代谢。Carba1 可用于癌症和化疗诱导的周围神经病变 (CIPN) 的研究。

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Carba1

Carba1 Chemical Structure

CAS No. : 2635394-10-2

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Carba1 is a bifunctional Carbazole (HY-D0204) derivative that activates nicotinamide phosphoribosyltransferase (NAMPT) and enhances NAD biosynthesis. Carba1 binds to colchicine site of tubulin, enhancing the anti-tumor effect of various chemotherapy drugs, such as Paclitaxel (HY-B0015). Carba1 exerts neuroprotective effect and can regulate cell energy metabolism. Carba1 can be used for the researches of cancer and chemotherapy-induced peripheral neuropathy (CIPN)[1].

体外研究
(In Vitro)

Carba1 (12 μM; 72 h) 与 Paclitaxel (HY-B0015)、Docetaxel (HY-B0011)、nab-Paclitaxel (HY-P99974) 和 Epothilone-B (HY-17029) 协同作用,抑制 HeLa 细胞的活力,使其 GI50 值降低 2.6,3.8, 1.8 和 4.4 倍[1]
Carba1 (1-20 μM; 60 mins) 增强 HeLa 细胞中 NAMPT 活性[1]
Carba1 (12 μM; 72 h) 保护成年小鼠 DRG 神经元免受 Paclitaxel、Cisplatin (HY-17394) 和 Bortezomib (HY-10227) 诱导的轴索变性,降低变性指数[1]
Carba1 (1-10 μM; 24 h) 在大鼠 DRG 神经元中对抗 Cisplatin 引起的神经毒性及髓鞘形成障碍[1]
Carba1 (12 μM, 2 h) 调节 HeLa 细胞代谢,升高乳酸、谷氨酸、ATP、GTP 水平,降低 NAD+ 水平,增强糖酵解和谷氨酰胺分解[1]

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

体内研究
(In Vivo)

Carba1 (50 mg/kg;腹腔注射;在第 0,1,2,4,7 和 9 天) 在 Paclitaxel 诱导大鼠神经病变模型中预防触觉异常性疼痛和神经退行性变[1]
Carba1 (60 mg/kg;静脉注射;每 2 天一次,共 10 天) 不会促进肿瘤生长,也不会抑制 Paclitaxel 在肿瘤生长模型中的抗肿瘤活性。[1]

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

Animal Model: Paclitaxel-induced rats neuropathy models[1]
Dosage: 50 mg/kg
Administration: Intraperitoneally injection; on days 0, 1, 2, 4, 7, 9
Result: Prevented tactile allodynia.
Reduced serum neurofilament light chain (NfL) levels.
Maintained intraepidermal nerve fiber (IENF) density.
分子量

294.78

Formula

C18H15ClN2

CAS 号
性状

固体

颜色

White to off-white

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
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  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
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Help & FAQs
  • 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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Carba1
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HY-179523
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