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Azimexon (BM 12.531) 是一种具有口服活性的免疫调节剂,具备辐射防护和抗肿瘤活性。Azimexon 可延长多种小鼠模型的生存期,增强免疫与造血功能,缓解辐射损伤和肿瘤转移。Azimexon 会在大鼠和犬中引发可逆性溶血性贫血,并对大鼠佐剂诱导性关节炎发挥治疗活性。Azimexon 可用于肺癌、白血病、多发性骨髓瘤、肺肿瘤、关节炎、乳腺癌以及艾滋病相关综合征的研究。

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Azimexon

Azimexon Chemical Structure

CAS No. : 64118-86-1

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Azimexon (BM 12.531) is an orally active immunomodulator with radioprotective and antitumor activities. Azimexon prolongs survival in multiple mouse models, enhances immunity and hematopoiesis, and alleviates radiation injury and tumor metastasis. Azimexon causes reversible hemolytic anemia in rats and dogs, and exerts therapeutic activity against adjuvant-induced arthritis in rats. Azimexon can be used for the research of lung carcinoma, leukemia, multiple myeloma, lung tumor, arthritis, breast cancer and AIDS‑related complex[1][2][3].

体外研究
(In Vitro)

Azimexon (0.01-4.0 μg/mL; 12 h) 在 0.01-0.25 μg/mL 浓度下可轻微增强 NK 细胞对 K562、IGR3 和 L1210 细胞的体外细胞毒性,在 1 μg/mL 以上浓度时则抑制 NK 活性[2]

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

体内研究
(In Vivo)

Azimexon (BM 12.531) (5-50 mg/kg;腹腔注射;第 0 天单次给药) 在剂量为 50 mg/kg 时,可使接受 500 R 全身照射的 CD2F1 小鼠达到 100% 存活率;而剂量为 20 mg/kg 时,可使接受 560 R 照射的小鼠达到 100% 存活率[1]
Azimexon (2.5-250 mg/kg;腹腔注射;第 0 天单次给药) 在 2.5 mg/kg 剂量下可显著增强正常 CD2F1 小鼠的迟发型超敏反应[1]
Azimexon (100 mg/kg;腹腔注射;第 9 天和第 16 天给药 2 次) 可使携带 M109 肺泡癌的 BALB/c 小鼠的平均存活时间显著延长[1]
Azimexon (50 mg/kg;腹腔注射;于第 8、11、13、15、18、20 天给药 6 次) 可显著增强 Cytoxan 对 CD2F1 小鼠 L1210 白血病的治疗效果[1]
Azimexon 与抗生素协同作用,可控制小鼠致死性细菌和真菌感染[2]
Azimexon 在小鼠肿瘤模型中表现出抗肿瘤作用[2]
Azimexon 可在小家鼠和褐家鼠中诱导多种免疫调节作用,包括白细胞增多、迟发型超敏反应激活以及巨噬细胞活化[2]
Azimexon 对 SD 大鼠的诱导性关节炎具有活性,并可通过增加集落形成单位来刺激骨髓[3]
Azimexon 可显著降低 X 射线对 SD 大鼠的毒性[3]
Azimexon (1-3 g/kg;口服、腹腔注射;单次给药) 的急性毒性较低,在小鼠中的口服 LD50 为 1 g/kg,在大鼠中为 3 g/kg,而在这两种物种中的腹腔注射 LD50 均为 1.5 g/kg[3]

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

Animal Model: CD2F1 (male, 6 to 10 weeks old, ~23 g, whole body X-ray irradiation at 500 R/560 R/590 R on day 0)[1]
Dosage: 5 mg/kg (500 R irradiation); 20 mg/kg (560 R/590 R irradiation); 50 mg/kg (500 R irradiation)
Administration: i.p.; single dose on day 0
Result: Achieved 90% survival and a mean survival time of 19.6 days at 5 mg/kg under 500 R irradiation.
Achieved 100% survival and a mean survival time of 20.0 days at 50 mg/kg under 500 R irradiation.
Achieved 100% survival and a mean survival time of 29.0 days at 20 mg/kg under 560 R irradiation without obvious body weight loss.
Showed no significant improvement in survival rate or mean survival time at 20 mg/kg under 590 R irradiation.
Animal Model: CD2F1 (male, 6 to 10 weeks old, ~23 g, delayed-type hypersensitivity assay via s.c. injection of 1 × 108 sheep red blood cells on day 0 and day 4)[1]
Dosage: 2.5 mg/kg; 25 mg/kg; 250 mg/kg
Administration: i.p.; single dose on day 0
Result: Increased footpad swelling by 0.55 mm (229% of SRBC control) at 2.5 mg/kg.
Increased footpad swelling by 0.33 mm (138% of SRBC control) at 25 mg/kg.
Increased footpad swelling by 0.33 mm (138% of SRBC control) at 250 mg/kg.
Animal Model: BALB/c (male, 6 to 10 weeks old, ~23 g, i.v. injection of 1 × 105 viable M109 alveolar carcinoma cells on day 0)[1]
Dosage: 100 mg/kg
Administration: i.p.; two doses on days 9 and 16
Result: Increased mean survival time from 13.2 days (untreated) to 17.4 days.
Resulted in 62% of treated mice surviving to day 16, compared to 0% of untreated mice.
Animal Model: CD2F1 (male, 6 to 10 weeks old, ~23 g, s.c. injection of 1 × 104 viable L1210 leukemia cells on day 0)[1]
Dosage: 50 mg/kg (single dose); 50 mg/kg (four doses); 50 mg/kg (six doses)
Administration: i.p.; single dose on day 8; four doses on days 8, 11, 13, 15; six doses on days 8, 11, 13, 15, 18, 20
Result: Increased mean survival time and survival rate at day 45 in a dose‑dependent manner following Cytoxan treatment, reaching 40.5 days and 70% with six 50 mg/kg doses.
分子量

194.23

Formula

C9H14N4O

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
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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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Azimexon
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HY-182506
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