TPCA-1
(Synonyms: 5-(4-氟苯基)-2-脲基噻吩-3-甲酰胺) 目录号 : GC17621
A selective inhibitor of IKK2
Cas No.:507475-17-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
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Cell lines |
Human Monocytes |
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Preparation method |
The solubility of this compound in DMSO is >14mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
0.1, 0.3, 1, 3 and 10 μM; 30 min |
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Applications |
In human peripheral blood monocytes, TPCA-1 inhibited the production of TNF-α, IL-6, and IL-8 induced by LPS in a concentration-dependent way with IC50 values of 170, 290, and 320 nM, respectively. |
| Animal experiment [1]: | |
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Animal models |
collagen-immunized/boosted DBA/1 mice |
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Dosage form |
3, 10, or 20 mg/kg, i.p., b.i.d., from days 1 to 48. |
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Application |
In collagen-immunized/boosted DBA/1 mice, TPCA-1 (20 or 10 mg/kg) dose-dependently reduced the severity of arthritis, resulting in a significantly decreased mean clinical score and delaying time to onset of disease. TPCA-1 (10 mg/kg, i.p., b.i.d.) also inhibited p65 nuclear localization and paw tissue levels of IL-1β, IL-6, TNF-α, and IFN-γ. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Podolin PL, Callahan JF, Bolognese BJ, Li YH, Carlson K, Davis TG, Mellor GW, Evans C, Roshak AK. Attenuation of murine collagen-induced arthritis by a novel, potent, selective small molecule inhibitor of IkappaB Kinase 2, TPCA-1 (2-[(aminocarbonyl)amino]-5-(4-fluorophenyl)-3 -thiophenecarboxamide), occurs via reduction of proinflammatory cytokines and antigen-induced T cell Proliferation. J Pharmacol Exp Ther. 2005 Jan;312(1):373-81. | |
TPCA-1 is a novel, potent, and selective inhibitor of human IKK-2.
Demonstration that IκB kinase 2 (IKK-2) plays a pivotal role in the nuclear factor-κB-regulated production of proinflammatory molecules by stimuli such as tumor necrosis factor (TNF)-α and interleukin (IL)-1 suggests that inhibition of IKK-2 may be beneficial in the treatment of rheumatoid arthritis.
In vitro: Determination of the activity of TPCA-1 against ten selected kinases, COX-1 and COX-2, showed the compound to be ~550-fold selective for IKK-2 versus ten of these enzymes. TPCA-1 inhibits lipopolysaccharide-induced human monocyte production of TNF-α, IL-6, and IL-8 with an IC50 of 170 to 320 nM [1].
In vivo: Prophylactic administration of TPCA-1 at 3, 10, or 20 mg/kg resulted in a dose dependent reduction in the severity of murine collagen-induced arthritis. The significantly reduced disease severity and delay of disease onset resulting from administration of TPCA-1 at 10 mg/kg were comparable to the effects of the antirheumatic drug, etanercept [1].
Clinical trial: No clinical data are available currently.
Reference:
[1] Podolin PL, Callahan JF, Bolognese BJ, Li YH, Carlson K, Davis TG, Mellor GW, Evans C, Roshak AK. Attenuation of murine collagen-induced arthritis by a novel, potent, selective small molecule inhibitor of IkappaB Kinase 2, TPCA-1 (2-[(aminocarbonyl)amino]-5-(4-fluorophenyl)-3 -thiophenecarboxamide), occurs via reduction of proinflammatory cytokines and antigen-induced T cell Proliferation. J Pharmacol Exp Ther. 2005 Jan;312(1):373-81.
| Cas No. | 507475-17-4 | SDF | |
| 别名 | 5-(4-氟苯基)-2-脲基噻吩-3-甲酰胺 | ||
| 化学名 | 2-(carbamoylamino)-5-(4-fluorophenyl)thiophene-3-carboxamide | ||
| Canonical SMILES | C1=CC(=CC=C1C2=CC(=C(S2)NC(=O)N)C(=O)N)F | ||
| 分子式 | C12H10FN3O2S | 分子量 | 279.29 |
| 溶解度 | ≥ 13.95mg/mL in DMSO, ≥ 2.53 mg/mL in EtOH with ultrasonic and warming | 储存条件 | Desiccate 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 | 3.5805 mL | 17.9025 mL | 35.8051 mL |
| 5 mM | 0.7161 mL | 3.5805 mL | 7.161 mL |
| 10 mM | 0.3581 mL | 1.7903 mL | 3.5805 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。