PKA Inhibitor Fragment (6-22) amide TFA

PKA Inhibitor Fragment (6-22) amide TFA is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide TFA can significantly reverse low-level morphine antinociceptive tolerance in mice.

Product information

Molecular Weight: 1982.08

Formula: C82H131F3N28O26

Synonym:

PKI-(6-22)-amide TFA

Chemical Name: (3S, 6S, 9S, 12S, 15S, 21S, 24S, 30S, 33S, 36S, 39S, 42S, 43S)-36-(2-amino-2-oxoethyl)-3-((S)-2-((S)-2-((2S, 3R)-2-amino-3-hydroxybutanamido)-3-(4-hydroxyphenyl)propanamido)propanamido)-6-benzyl-9-sec-butyl-42-carbamoyl-21, 30, 33-tris(3-guanidinopropyl)-24-((R)-1-hydroxyethyl)-15-(hydroxymethyl)-12, 39, 43-trimethyl-4, 7, 10, 13, 16, 19, 22, 25, 28, 31, 34, 37, 40-tridecaoxo-5, 8, 11, 14, 17, 20, 23, 26, 29, 32, 35, 38, 41-tridecaazapentatetracontan-1-oic acid compound with 2, 2, 2-trifluoroacetic acid (1:1)

Smiles: C[C@@H](O)[C@H](NC(=O)[C@H](CCCNC(N)=N)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CC1C=CC=CC=1)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](C)NC(=O)[C@H](CC1C=CC(O)=CC=1)NC(=O)[C@@H](N)[C@@H](C)O)[C@@H](C)CC)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H]([C@@H](C)CC)C(N)=O.OC(=O)C(F)(F)F

InChiKey: LIWOHBLBMLDFEF-HMPYOKLMSA-N

InChi: InChI=1S/C80H130N28O24.C2HF3O2/c1-10-37(3)60(63(83)118)106-66(121)41(7)96-72(127)52(32-55(81)113)103-69(124)49(22-17-29-92-80(88)89)100-68(123)47(20-15-27-90-78(84)85)98-57(115)35-94-76(131)62(43(9)111)108-70(125)48(21-16-28-91-79(86)87)99-56(114)34-93-67(122)54(36-109)105-65(120)40(6)97-77(132)61(38(4)11-2)107-74(129)51(30-44-18-13-12-14-19-44)102-73(128)53(33-58(116)117)101-64(119)39(5)95-71(126)50(104-75(130)59(82)42(8)110)31-45-23-25-46(112)26-24-45;3-2(4,5)1(6)7/h12-14,18-19,23-26,37-43,47-54,59-62,109-112H,10-11,15-17,20-22,27-36,82H2,1-9H3,(H2,81,113)(H2,83,118)(H,93,122)(H,94,131)(H,95,126)(H,96,127)(H,97,132)(H,98,115)(H,99,114)(H,100,123)(H,101,119)(H,102,128)(H,103,124)(H,104,130)(H,105,120)(H,106,121)(H,107,129)(H,108,125)(H,116,117)(H4,84,85,90)(H4,86,87,91)(H4,88,89,92);(H,6,7)/t37-,38-,39-,40-,41-,42+,43+,47-,48-,49-,50-,51-,52-,53-,54-,59-,60-,61-,62-;/m0./s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: H2O : 50 mg/mL (25.23 mM; Need ultrasonic)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

References:

1. Katz BM, et, al. Synthesis, characterization and inhibitory activities of (4-N3[3,5-3H]Phe10)PKI(6-22)amide and its precursors: photoaffinity labeling peptides for the active site of cyclic AMP-dependent protein kinase. Int J Pept Protein Res. 1989 Jun;33(6):439-45.
2. Dalton GD, et, al. Alterations in brain Protein Kinase A activity and reversal of morphine tolerance by two fragments of native Protein Kinase A inhibitor peptide (PKI). Neuropharmacology. 2005 Apr; 48(5): 648-57.

Products are for research use only. Not for human use.