| Bioactivity | TAK-639, a topical C-type natriuretic peptide analog, is a selective and potent natriuretic peptide receptor B (NPR-B) agonist with an EC50 of 61 nM. TAK-639 is an efficacious intraocular pressure (IOP) lowering agent[1]. |
| Target | EC50: 61 nM (NPR-B), 2179 nM (NPR-A) |
| Invitro | TAK-639 has an IC50 of 8.2 μM, equivalent to a Ki of 6.6 μM for the AT2 receptor; and an IC50 of 25.8 μM, equivalent to a Ki of 16.2 μM for the CCK1 receptor[1].TAK-639 (15 or 25 min) activates NPR-B dose-dependently with an EC50 of 61 ± 3 nM in GTM-3 cells, and activates NPR-A with an EC50 of 2179 ± 386 nM in 293-T cells[1]. |
| In Vivo | TAK-639 (0.1%-0.6%; topical ocular; 5 μL) significantly lowers IOP in the treated eye in mice[1]. Animal Model: |
| Name | TAK-639 |
| Formula | C65H110ClN13O13 |
| Molar Mass | 1317.10 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Millar JC, et al. Effects of TAK-639, a novel topical C-type natriuretic peptide analog, on intraocular pressure and aqueous humor dynamics in mice. Exp Eye Res. 2019 Nov;188:107763. |