BA 1 TFA is a potent agonist for the bombesin (BB) family of receptors. BA1 binds with high affinity to Bombesin receptor subtype-3 (BRS3), gastrin releasing peptide receptor (GRPR), neuromedin B receptor (NMBR) with IC50s of 6, 0.4, 2.5 nM[1].
2.;;Calculate the overall charge of the entire peptide according to the following table:
;
Contents
Assign value
Acidic amino acid
Asp (D), Glu (E), and the C-terminal -COOH.
-1
Basic amino acid
Arg (R), Lys (K), His (H), and the N-terminal -NH2
+1
Neutral amino acid
Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q)
0
3.;;Recommended solution:
Overall charge of peptide
Details
Negative (lt;0)
1.;;Try to dissolve the peptide in water first. 2.;;If water fails, add NH4OH (lt;50 μL). 3.;;If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
Positive (gt;0)
1.;;Try to dissolve the peptide in water first. 2.;;If water fails, try dissolving the peptide in a 10%-30% acetic acid solution. 3.;;If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO.
Zero (=0)
1.;;Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first. 2.;;For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration.
参考文献
[1]. Terry W Moody, et al. ML-18 is a non-peptide bombesin receptor subtype-3 antagonist which inhibits lung cancer growth. Peptides. 2015 Feb;64:55-61.
Urotensin I (Catostomus urotensin I), a CRF-like neuropeptide, acts as an agonist of CRF receptor with pEC50s of 11.46, 9.36 and 9.85 for human CRF1, human CRF2 and rat CRF2α receptors in CHO cells, and Kis of 0.4, 1.8, and 5.7 nM for hCRF1, rCRF2α and mCRF2β receptors, respectively[1][2].
IC50 Target
pEC50: 11.46 (human CRF1, CHO cells), 9.36 (human CRF2, CHO cells), 9.85 (rat CRF2α, CHO cells)[1] Ki: 0.4 nM (hCRF1, cell assay), 1.8 nM (rCRF2α, cell assay), and 5.7 nM (mCRF2β, cell assay)[2]
体外研究 (In Vitro)
Urotensin I is 2-3 times more potent than CRF or sauvagine in stimulating ACTH release from a superfused goldfish anterior pituitary cell column[3]. Rat tail artery strips were incubated in the presence of 4 x 10(-3) M theophylline and Urotensin I (UI). At the concentrations of 1.50, 7.50 mU/ml but not of 0.75 mU/ml Urotensin I, the content of cAMP increased significantly[4].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
Intraperitoneal injections of urotensin I, a CRF-like neuropeptide isolated from the caudal neurosecretory system of the teleost Catostomus commersoni, ovine CRF and sauvagine all produced significant increases in circulating levels of plasma cortisol in goldfish in which endogenous ACTH secretion was suppressed with betamethasone[3].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.