TAK-683 acetate
PRODUCTS SPECIFICATIONS
DESCRIPTION
Overview
| MDL | - |
|---|---|
| Molecular Weight | 1358.50 |
| Molecular Formula | C66H87N17O15 |
| SMILES | - |
Summary
TAK-683 acetate is a potent full KISS1 receptor (KISS1R) agonist ( IC 50 =170 pM) with improved metabolic stability. TAK-683 acetate is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC 50 values of 0.96 nM and 1.6 nM for human and rat, respectively [1] . TAK-683 acetate depletes GnRH in the hypothalamus and reduces plasma FSH , LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer [1] [2] [4] .
In Vitro
TAK-683 acetate exhibits an IC
50
value (95% CI) from receptor binding assays is 150-180 pM and EC
50
value (95% CI) from Ca
+
mobilization assays is 180 (159–203) pM in rat KISS1R-expressing Chinese hamster ovary (CHO) cells
[4]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
TAK-683 acetate (subcutaneous injection; 0.008, 0.08, 0.8, or 8 μmol/ml/kg; once daily; 7 days) induces an increase in plasma luteinizing hormone and testosterone levels; however, after day 7, plasma hormone levels and genital organ weights are reduced
[3]
.
TAK-683 acetate (subcutaneous injection; 10, 30, or 100 pmol/h; once daily; 4 weeks) provides a promising for suppressing reproductive functions and hormone-related diseases such as prostate cancer
[3]
.
TAK-683 acetate (subcutaneous injection; 2.1-21 nmol/kg/day; once daily; 12 weeks) has a longer-term evaluation in prostate cancer model, serum concentrations of PSA is reduced in rats, PSA concentrations are reduced to below the limit of detection (0.5 ng/ml)) in all rats by day 14
[4]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male SD rat with prostate cancer model [4] |
| Dosage: | 2.1, 7, 14, 21 nmol/kg/day |
| Administration: | Subcutaneous injection |
| Result: | Exhibited a sustained testosterone suppression in rat. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Sealed storage, away from moisture and light, under nitrogen
| Powder | -80°C | 2 years |
|---|---|---|
| -20°C | 1 year |
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)
Solvent & Solubility
H 2 O : 5 mg/mL ( 3.68 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 0.7361 mL | 3.6805 mL | 7.3611 mL |
| 5 mM | --- | --- | --- |
| 10 mM | --- | --- | --- |
References
- [1] Nishizawa N, et al. Design and Synthesis of an Investigational Nonapeptide KISS1 Receptor (KISS1R) Agonist, Ac-d-Tyr-Hydroxyproline (Hyp)-Asn-Thr-Phe-azaGly-Leu-Arg(Me)-Trp-NH2 (TAK-448), with Highly Potent Testosterone-Suppressive Activity and Excellent Water Solubility. J Med Chem. 2016 Oct 13;59(19):8804-8811. Epub 2016 Sep 21.
- [2] Asami T, et al.Design, synthesis, and biological evaluation of novel investigational nonapeptide KISS1R agonists with testosterone-suppressive activity.J Med Chem. 2013 Nov 14;56(21):8298-307.
- [3] Hisanori MATSUI, et al. Functional Analyses of Kisspeptin in Controlling Gonadal Functions