K41498
Based on 1 Customer Validation
K41498 is a highly selective CRF 2 receptor antagonist, with a Ki of 0.66 nM for human CRF2α receptor and a Ki of 0.62 nM for human CRF2β receptor. K41498 inhibits cAMP accumulation in cells expressing CRF2. K41498 antagonizes the hypotensive response induced by systemic administration of urocortin in conscious rats. K41498 undergoes radioiodination without loss of activity and serves for autoradiographic studies of native CRF2 receptors in rat brain and peripheral tissues.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.66%
- CAS 番号: 434938-41-7
- 分子式: C162H276N48O46
- 分子量:3632.20
-
保管条件:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
生物活性
|
CRFR2 |
K41498 (incubated at 22°C for 120 min) exhibits highly selective and high-affinity binding to hCRF2α and hCRF2β receptors in membrane homogenates of stably transfected HEK293 cells (Ki = 0.66 nM and 0.62 nM, respectively), which is significantly superior to its binding to hCRF1 receptor[1].
K41498 (10 μM in hCRF1-expressing cells; 100 nM in hCRF2α- and hCRF2β-expressing cells; treated at 37°C for 10 min) is a potent, selective antagonist that inhibits cAMP accumulation in Svg-stimulated HEK293 cells expressing hCRF2α and hCRF2β. It exhibits only extremely low intrinsic agonist activity across all three receptor subtypes and shows weak activity at the hCRF1 receptor[1].
K41498 (100 nM, 10 min at 37°C for CRF2α/CRF2β cells; 10 μM, 10 min at 37°C for CRF1 cells) potently inhibits sauvagine-induced cAMP accumulation in HEK293 cells expressing human CRF2α and human CRF2β at a concentration of 100 nM, shows only weak inhibitory effect on HEK293 cells expressing human CRF1 at a concentration of 10 μM, and exhibits only extremely low intrinsic agonist activity in all three of the above-mentioned cell lines[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
K41498 (1.84 mg; i.v.; single administration, 10 minutes prior to urocortin administration) completely blocks the systemic urocortin-induced hypotensive response in conscious male Wistar-Kyoto rats, whereas K41498 (2.35 mg; i.c.v.; single administration, 10 minutes prior to urocortin administration) fails to block the pressor effect induced by urocortin[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:BALB/c nude (9-week-old female, 18-25 g)[1]
-
Dosage:1 mg/kg
-
Administration:i.v.; single dose
-
Result:Reduced specific uptake of 123I-K31440 in the small intestine by 35%.
-
Animal Model:Wistar-Kyoto rats (male, 340-360 g)[2]
-
Dosage:1.84 mg (systemic administration); 2.35 mg (central administration)
-
Administration:i.v.; single dose, 10 minutes prior to urocortin; i.c.v.; single dose, 10 minutes prior to urocortin
-
Result:Completely abolished the >30 mmHg hypotensive response evoked by systemic urocortin .
Did not alter the pressor response evoked by central urocortin.
化学情報
-
CAS 番号 434938-41-7
-
性状 Solid
-
分子量 3632.20
-
分子式 C162H276N48O46
-
Color White to off-white
-
配列
{D-Phe}-His-Leu-Leu-Arg-Lys-{Nle}-Ile-Glu-Ile-Glu-Lys-Gln-Glu-Lys-Glu-Lys-Gln-Gln-Ala-Ala-Asn-Asn-Arg-Leu-Leu-Leu-Asp-Thr-Ile-NH2
-
シーケンスの短縮
{D-Phe}-HLLRK-{Nle}-IEIEKQEKEKQQAANNRLLLDTI-NH2
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶剤 & 溶解度
H2O : 50 mg/mL (13.77 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
-
データシート (284 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
取扱説明書 (2659 KB)
参考文献
[1]. Rühmann A, et al. Design, synthesis and pharmacological characterization of new highly selective CRF(2) antagonists: development of 123I-K31440 as a potential SPECT ligand. Peptides. 2002;23(3):453-460. [Content Brief]
[2]. Lawrence AJ, et al. The highly selective CRF(2) receptor antagonist K41498 binds to presynaptic CRF(2) receptors in rat brain. Br J Pharmacol. 2002 Jul;136(6):896-904. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 0.2753 mL | 1.3766 mL | 2.7532 mL | 6.8829 mL |
| 5 mM | 0.0551 mL | 0.2753 mL | 0.5506 mL | 1.3766 mL | |
| 10 mM | 0.0275 mL | 0.1377 mL | 0.2753 mL | 0.6883 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
K41498 関連分類
HY-P1106 関連分類
Powered by Bioz