TPCA-1 is an inhibitor of IKK-2 with IC50 of 17.9 nM.
AAPS PharmSciTech. 2020 Nov 2;21(8):298.
Targeted and Combined TPCA-1-Gold Nanocage Therapy for In Vivo Treatment of Inflammatory Arthritis
TPCA-1 purchased from AbMole
Pharmaceutics. 2019 Mar 25;11(3).
Hyaluronic Acid-Modified and TPCA-1-Loaded Gold Nanocages Alleviate Inflammation.
TPCA-1 purchased from AbMole
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Source | AAPS PharmSciTech (2020 Nov), Figure 3, TPCA-1 (Abmole Bioscience Inc. Houston, TX, USA) |
| Method | TPCA-1-treated | |
| Cell Lines | mice | |
| Concentrations | 0.016 mg/kg | |
| Incubation Time | 6 days | |
| Results | AuNCs/T/P and HA-AuNCs/T/P treatment significantly reduced the clinical arthritis score and swelling of the hind paws compared with untreated and TPCA-1-treated mice. |
| Molecular Weight | 279.29 |
| Formula | C12H10FN3O2S |
| CAS Number | 507475-17-4 |
| Solubility (25°C) | DMSO 36 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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