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T2955

Sigma-Aldrich

γ6 TM1a trifluoroacetate salt

≥95% (HPLC)

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Synonym(s):
LGLLVAIV trifluoroacetate salt, Leu-Gly-Leu-Leu-Val-Ala-Ile-Val trifluoroacetate salt
Empirical Formula (Hill Notation):
C39H72N8O9 · xC2HF3O2
CAS Number:
Molecular Weight:
797.04 (free base basis)
MDL number:
PubChem Substance ID:
NACRES:
NA.77

assay

≥95% (HPLC)

form

lyophilized powder

solubility

H2O: >1 mg/mL

storage temp.

−20°C

SMILES string

OC(=O)C(F)(F)F.CC[C@H](C)[C@H](NN[C@@H](C(C)C)C(O)=O)C(=O)N[C@H](C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(C)C)C(=O)C(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@@H](N)CC(C)C

InChI

1S/C39H72N8O9.C2HF3O2/c1-14-24(12)32(47-46-31(23(10)11)39(55)56)38(54)42-25(13)35(51)45-30(22(8)9)37(53)44-28(17-21(6)7)34(50)33(49)27(16-20(4)5)43-29(48)18-41-36(52)26(40)15-19(2)3;3-2(4,5)1(6)7/h19-28,30-32,46-47H,14-18,40H2,1-13H3,(H,41,52)(H,42,54)(H,43,48)(H,44,53)(H,45,51)(H,55,56);(H,6,7)/t24-,25+,26-,27-,28-,30-,31-,32-;/m0./s1

InChI key

YOPDKLRUJCDCMP-AFAMYAHFSA-N

Amino Acid Sequence

Leu-Gly-Leu-Leu-Val-Ala-Ile-Val

Biochem/physiol Actions

The calcium channel γ family is a subgroup of the tetraspanin proteins. There are the eight γ subunits that have been identified to date. Among these γ1 subunit acts as an endogenous antagonist of the skeletal HVA calcium current, and γ6 inhibits the low voltage-activated (LVA) Cav3.1 calcium current. A GxxxA motif in the first transmembrane domain (TM1) of γ6 was identified as critical for inhibiting the Cav3.1 current. γ6 TM1a is an octapeptide contains residues 41 through 48 of the native γ6 protein. The peptide inhibits the Cav3.1 calcium current in a dose-dependent manner. The reduction of channel current is mostly due to the inhibition of both resting and inactivated channels relatively independent of membrane potential. Thus γ6 TM1might function as a pore blocker. Also γ6 TM1a peptide inhibits Cav1.2 current with reduced efficacy. The γ6 TM1a peptide has the potential of being further developed as a novel therapeutic agent targeting Cav3.1 and possibly Cav1.2 calcium current.

Features and Benefits

This compound is featured on the Calcium Channels page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Preparation Note

γ6 TM1a trifluoroacetate salt is soluble in water at a concentration that is greater than 1 mg/ml.

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_c

Not applicable


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