K41498 TFA

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K41498 TFA;

K41498 TFA 是一种强选择性的 CRF2 receptor 拮抗剂，其对人 CRF2α、CRF2β 和 CRF1 受体的 Ki 值分别为 0.66 nM、0.62 nM和425 nM。K41498 TFA 是 antisauvagine-30 (aSvg-30) 的类似物，可抑制 sauvagine 刺激的 cAMP 在 hCRF2α/hCRF2β 表达细胞中的积累。K41498 可用于低血压研究。

K41498 TFAamp;;

K41498 TFA Chemical Structure

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生物活性

K41498 TFA is a potent and highly selective CRF2 receptor antagonist with Ki values of 0.66 nM, 0.62 nM and 425 nM for human CRF2α, CRF2β and CRF1 receptors respectively. K41498 TFA is an analogues of antisauvagine-30 (aSvg-30), inhibits sauvagine-stimulated cAMP accumulation in hCRF2α– and hCRF2β-expressing cells. K41498 TFA can be used for hypotension study[1].

分子量

3746.22

Formula

C164H277F3N48O48
Sequence

{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
Sequence Shortening

{D-Phe}-HLLRK-{Nle}-IEIEKQEKEKQQAANNRLLLDTI-NH2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. A Rühmann, 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 Mar;23(3):453-60.

    [2]. A J Lawrence, et al. The highly selective CRF(2) receptor antagonist K41498 binds to presynaptic CRF(2) receptors in rat brain. Br J Pharmacol