TOK-8801
目录号 : GC31957
TOK-8801是一种合成的二氢咪唑并噻唑羧酰胺，正在开发作为免疫调节剂。
Cas No.:105963-46-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | Spleen cells (2×105) or thymus cells (2×105) from BALB/c mice are cultured with Con A (1 or 5 μg/mL) or LPS (10 μg/mL) in 0.2 mL of RPMI-1640 medium containing 5% FCS using round-bottomed microculture plates with 96 wells for 2 days and are pulsed with 0.5 μCi of 3H-TdR for an additional 18 hr. Then, cells are harvested on glass fiber fillters, and 3H-TdR incorporation is measured in a liquid scintillation counter. TOK-8801 is added at the initiation of the culture[1]. |
Animal experiment: | Male BDFI mice are used in this study. Control mice are maintained without food or water while counterparts are under the condition of restraint-stress. On the next day, the mice are immunized with 5×108 SRBC intraperitoneally. Immediately, 24 hr and 48 hr after the immunization, TOK-8801 is orally given at doses of 0.02, 0.1 and 0.5 mg/kg/day. All administrations are done after a starvation for 6 hr. Four days after the immunization, splenic anti SRBC PFC are assayed[1]. |
References: [1]. Fujiwara M, et al. Immunomodulatory activity of the newly synthesized compound TOK-8801 (N-(2-phenylethyl)-3,6,6-trimethyl-5,6-dihydroimidazo[2,1-b]thiazole-2- carboxamide). Jpn J Pharmacol. 1989 Dec;51(4):549-54. | |
TOK-8801 is a synthesized dihydroimidazothiazole carboxamide and is under development as an immunomodulator.
TOK-8801 is a synthesized dihydroimidazothiazole carboxamide and is under development as an immunomodulator. TOK-8801 augments the in vitro anti-SRBC PFC response of murine splenocytes in a bell-shaped manner. The stimulatory effect of TOK-8801 is observed at concentrations of 2.5×10-7 to 2.5×10-5 M and is diminished at 10-4 M. The cell-viability is not altered during the culture with TOK-8801 at any doses used in this experiment (10-7 to 10-4 M). TOK-8801 enhances the 3H-TdR uptake of these responses in a bell-shaped manner, and effective concentrations of TOK-8801 are 10-7 to 10-5 M[1].
The anti-SRBC PFC response per spleen, which is prominently lowered by restraint-stress (P<0.05), is significantly restored by the administration of TOK-8801 (0.5 mg/kg, P<0.05). The number of total splenic lymphocytes in restraint-stress is decreased, but there are no significant changes in the number of total splenic lymphocytes by the treatment with TOK-8801[1]. When TOK-8801 is administered orally at doses of 0.1 to 10 mg/kg, the number of plaque forming cell (PFC) significantly decreases or tends to decrease. Treatment of TOK-8801 at doses of 0.1 to 1 mg/kg causes significant suppression in the delayed-type hypersensitivity (DTH) reaction induced in high responder[2].
[1]. Fujiwara M, et al. Immunomodulatory activity of the newly synthesized compound TOK-8801 (N-(2-phenylethyl)-3,6,6-trimethyl-5,6-dihydroimidazo[2,1-b]thiazole-2- carboxamide). Jpn J Pharmacol. 1989 Dec;51(4):549-54. [2]. Shibata K, et al. Immunomodulatory effect of a newly synthesized compound, TOK-8801 (N-(2-phenylethyl)-3,6,6-trimethyl-5,6-dihydroimidazo [2,1-b]thiazole-2-carboxamide) on antibody production in vivo and delayed-type hypersensitivity in mice. Int J Immunopharmacol. 1990;12(5):497-502.
| Cas No. | 105963-46-0 | SDF | |
| Canonical SMILES | O=C(C1=C(C)N2C(S1)=NC(C)(C)C2)NCCC3=CC=CC=C3 | ||
| 分子式 | C17H21N3OS | 分子量 | 315.43 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1703 mL | 15.8514 mL | 31.7028 mL |
| 5 mM | 0.6341 mL | 3.1703 mL | 6.3406 mL |
| 10 mM | 0.317 mL | 1.5851 mL | 3.1703 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Immunomodulatory activity of the newly synthesized compound TOK-8801 (N-(2-phenylethyl)-3,6,6-trimethyl-5,6-dihydroimidazo[2,1-b]thiazole-2- carboxamide)
The in vitro and in vivo effects of the newly synthesized compound TOK-8801 (N-(2-phenylethyl)-3,6,6-trimethyl-5,6-dihydroimidazo[2,1-b] thiazole-2-carboxamide) on immune responses were investigated in comparison with that of levamisole (LMS). TOK-8801 enhanced the anti-sheep red blood cells (SRBC) plaque forming cells (PFC) response and mitogen-induced proliferative responses in murine splenocytes and thymocytes in vitro at concentrations of 10(-7)-10(-5) M, while LMS augmented these responses at 10(-4) M. The stimulatory effect of TOK-8801 as well as LMS on the antibody production was eliminated by the removal of T cells. TOK-8801 (0.5 mg/kg, p.o.) suppressed the in vivo generation of anti-SRBC PFC in normal mice, but the compound restored the depressed antibody production in restraint-stress mice which was mainly caused by helper T cell defects. From these results, TOK-8801 was shown to have an immunomodulatory activity in the antibody production.
Immunomodulatory effect of a newly synthesized compound, TOK-8801 (N-(2-phenylethyl)-3,6,6-trimethyl-5,6-dihydroimidazo [2,1-b]thiazole-2-carboxamide) on antibody production in vivo and delayed-type hypersensitivity in mice
The immunopharmacological effects of a newly synthesized compound in vivo, TOK-8801 (N-(2-phenylethyl)-3,6,6-trimethyl-5,6-dihydroimidazo[2,1-b]thi azo le-2- carboxamide), on the anti-SRBC plaque-forming cell (PFC) response and delayed-type hypersensitivity (DTH) reaction were investigated. Oral administration of TOK-8801 (0.1-10 mg/kg) resulted in the suppression of the PFC responses to varying doses of antigen (5 x 10(6), 2 x 10(7), 1 x 10(8)) in C3H/He strain mice (7 W) which are high responders to SRBC antigen. On the other hand, the compound augmented the PFC response in aged mice (8-9 months) in which the PFC response was markedly depressed compared with that in young mice. In the experiment of the methylated human serum albumin-induced DTH reaction, TOK-8801 augmented the reaction in low responder (C57BL/6) mice by oral administrations of 0.1-1 mg/kg for 5 days from the sensitization, whereas suppressed the reaction in high responder (ICR) mice. These immunopharmacological actions of TOK-8801 were compared in dose and activity with those of lobenzarit and bucillamine. Thus, these results suggest that TOK-8801 may act as an immunomodulating agent and would be expected to be a useful agent for autoimmune diseases such as rheumatoid arthritis.