1. GPCR/G Protein Neuronal Signaling
  2. Neuropeptide Y Receptor
  3. Galantide

Galantide, a non-specific galanin receptor antagonist, is a peptide consisting of fragments of galanin and substance P. Galantide recognizes two classes of galanin binding sites (KD<0.1 nM and ~6 nM) in the rat hypothalamus. Galantide dose dependently (IC50=1.0 nM) antagonizes the galanin-mediated inhibition of the glucose-induced insulin secretion from mouse pancreatic islets. Galantide appears to bind to a single population of SP receptors (KD~40 nM).

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Galantide TFA) usually boasts enhanced water solubility and stability.

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Galantide

Galantide 構造式

CAS 番号 : 138579-66-5

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製品説明

Galantide, a non-specific galanin receptor antagonist, is a peptide consisting of fragments of galanin and substance P. Galantide recognizes two classes of galanin binding sites (KD<0.1 nM and ~6 nM) in the rat hypothalamus. Galantide dose dependently (IC50=1.0 nM) antagonizes the galanin-mediated inhibition of the glucose-induced insulin secretion from mouse pancreatic islets. Galantide appears to bind to a single population of SP receptors (KD~40 nM)[1][2][3].

体外実験

Galantide do not activate the K+ conductance but produces a concentration-dependent antagonism (IC50=4 nM) of the galanin-induced increase in K+ conductance. Galantide acts like galanin and inhibits the voltage-dependent Ba2+ current (IBa). The inhibition of IBa also is concentration dependent (IC50=16 nM) and the maximum inhibition produced by galantide is approximately 40%[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

体内実験

Intracerebroventricular injection of galanin (5 micrograms/rat) inhibited sexual behavior in experienced male rats--without producing any other locomotor or behavioral deficit-, injection of the galanin antagonist, galantide, by the same route (1 or 2 micrograms/rat) stimulated sexual behavior (improving arousal, motivation and performance indexes) and antagonized the effect of galanin[2]. Galantide ameliorates mild acute pancreatitis (AP). Galantide significantly reduces AP-induced hyperenzymemia by 41–49%[3]. Galantide has been found to improve social memory in 'socialrecognition' test when i.c.v. administered at doses varying from 6-6000 nM[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

2199.53

分子式

C104H151N25O26S

CAS 番号
Appearance

Solid

Color

White to off-white

Sequence

Gly-Trp-Thr-Leu-Asn-Ser-Ala-Gly-Tyr-Leu-Leu-Gly-Pro-Gln-Gln-Phe-Phe-Gly-Leu-Met-NH2

Sequence Shortening

GWTLNSAGYLLGPQQFFGLM-NH2

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Sealed storage, away from moisture
Powder -80°C 2 years
  -20°C 1 year
In solvent -80°C 6 months
  -20°C 1 month
純度とドキュメンテーション
参考文献
動物実験
[3][4]

Rats: Galantide is dissolved in 0.9% NaCl. The i.c.v. injection is given to the resident rat immediately after removal of the juvenile, at the end of the first encounter. Control rats receive an equal volume (4 µL) of saline by the same route, at the same infusion rate (1 µL/20 s) and at the same time. A minimum of 10 adult rats are used for each dose level[4].

Mice: Galantide stock solution is prepared in 0.01% bovine serum albumin in saline. The mice are allocated to 7 groups: Mice administered the vehicle for injection (saline alone), mice administered only caerulein (AP alone), mice administered only galantide (GT alone) or feG (feG alone), mice administered caerulein and galantide (AP+GT) or caerulein and feG (AP+feG) and finally mice that are administered with caerulein, galantide and feG (AP+GT+feG). On the day prior to the AP induction, a blood sample is collected to measure the basal plasma amylase activity[3].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。

参考文献
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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製品名:
Galantide
製品番号:
HY-P0262
数量:
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