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G113

Sigma-Aldrich

GR 64349

>96%

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Empirical Formula (Hill Notation):
C42H68N10O11S
CAS Number:
137593-52-3
Molecular Weight:
921.11
PubChem Substance ID:
329799740
NACRES:
NA.32

Assay

>96%

storage temp.

−20°C

SMILES string

CSCC[C@H](NC(=O)[C@H](CC(C)C)N1CC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@@H](N)CCCCN)C(C)C)C1=O)C(N)=O

InChI

1S/C42H68N10O11S/c1-23(2)19-32(40(61)46-27(35(45)56)15-18-64-5)52-17-14-28(42(52)63)47-41(62)34(24(3)4)51-38(59)29(20-25-11-7-6-8-12-25)49-39(60)31(22-53)50-37(58)30(21-33(54)55)48-36(57)26(44)13-9-10-16-43/h6-8,11-12,23-24,26-32,34,53H,9-10,13-22,43-44H2,1-5H3,(H2,45,56)(H,46,61)(H,47,62)(H,48,57)(H,49,60)(H,50,58)(H,51,59)(H,54,55)/t26-,27-,28-,29-,30-,31-,32-,34-/m0/s1

InChI key

HVUNRXRFMQDMBO-NOJSRKIXSA-N

Gene Information

human ... TACR2(6865)
mouse ... TACR2(21337)
rat ... TACR2(25007)

Amino Acid Sequence

Lys-Asp-Ser-Phe-Val-Gly-R-γ-lactam-Leu-Met-NH2

General description

Neurokinin (NK) receptors are acted upon by tachykinins or neurokinins namely, NKA and NKB. These are endogenous ligands. An exogenous agonist/ligand for NK2 is GR 64349 peptide.

Biochem/physiol Actions

GR 64349 peptide acts as an agonist of neurokinin (NK2) receptor, which leads to reduced NK2 response to kainate and AMPA (α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid), but not to NMDA (N-methyl-D-aspartate).

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Personal Protective Equipment

dust mask type N95 (US), Eyeshields, Gloves

Regulatory Information

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Lesley Marson et al.
European journal of pharmacology, 819, 261-269 (2017-12-15)
The suitability of various neurokinin-2 (NK2) receptor agonists and routes of administration to elicit on-demand voiding of the bladder and bowel, as future therapy for individuals with spinal cord injury, was examined using a rat model. The current study examined
Rajesh Gour et al.
European journal of medicinal chemistry, 178, 552-570 (2019-06-20)
We report herein the synthesis and anticancer activity of a set of novel S-linked artemisinins bearing an aliphatic/aromatic/heterocyclic nucleus as a substituent on the sulfur. The compounds were prepared from artemisinin via its lactol-form by an acid-catalyzed condensation of the
B A Chizh et al.
British journal of pharmacology, 115(6), 1013-1019 (1995-07-01)
1. The effects of selective tachykinin (neurokinin, NK) NK1 and NK2 receptor antagonists have been examined on spinal neurones in alpha-chloralose anaesthetized, spinalized rats. They were tested for effects on responses both to excitatory amino acids (EAA) and to noxious
S Guard et al.
Neurochemistry international, 18(2), 149-165 (1991-01-01)
The use of selective agonists in both functional and binding studies has provided unequivocal evidence for the existence of three types of tachykinin receptor (NK(1), NK(2) and NK(3)); there is also preliminary evidence for the existence of further subtypes. These
R M Hagan et al.
Neuropeptides, 19(2), 127-135 (1991-06-01)
The pharmacological profiles of two novel neurokinin agonists have been investigated. delta Ava[L-Pro9,N-MeLeu10]SP(7-11) (GR73632) and [Lys3,Gly8-R-gamma-lactam-Leu9] NKA(3-10) (GR64349) are potent and selective agonists at NK-1 and NK-2 receptors respectively. In the guinea-pig isolated trachea preparation, contractions induced by these agonists

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