GR 64349 TFA

GR 64349 TFA;

GR 64349 是有效的、高度选择性的神经激肽 2 (NK2) 受体的肽类拮抗剂,其在大鼠结肠中测得的EC50 值为 3.7 nM。GR 64349 对 NK1 和 NK3 受体的选择性要低 1000 和 300 倍以上。

GR 64349 TFAamp;;

GR 64349 TFA Chemical Structure

规格 是否有货
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生物活性

GR 64349 is a potent and highly selective NK2 receptor peptide antagonist, with an EC50 of 3.7 nM in rat colon. GR 64349 exhibits selectivity >1000 and >300-fold with respect to NK1 and NK3 receptors, respectively[1][2].

分子量

1035.13

Formula

C44H69F3N10O13S

Sequence Shortening

KDSFV{Aaa}LM-NH2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Y Chang, et al. Tachykinin receptor subtypes in the isolated guinea pig heart and their role in mediating responses to neurokinin A. J Pharmacol Exp Ther. 2000 Jul;294(1):147-54.

    [2]. M J Deal, et al. Conformationally constrained tachykinin analogues: potent and highly selective neurokinin NK-2 receptor agonists. J Med Chem. 1992 Oct 30;35(22):4195-204.

GR 94800 TFA

GR 94800 TFA;

GR 94800 TFA 是有效的、选择性的神经激肽 2 (NK2) 受体的肽类拮抗剂,其对 NK2、NK1 和 NK3 受体的 pKB 值分别为 9.6、6.4 和 6.0。

GR 94800 TFAamp;;

GR 94800 TFA Chemical Structure

规格 是否有货
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250 mg ; 询价 ;
500 mg ; 询价 ;

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生物活性

GR 94800 TFA is a potent and selective NK2 receptor peptide antagonist, with pKB values of 9.6, 6.4 and 6.0 for NK2, NK1 and NK3 receptors, respectively[1][2].

体外研究
(In Vitro)

Responses to EFS (15 Hz) were significantly reduced by the NK2 receptor antagonist GR 94800 (1 μM) either alone or in combination with the NK1 antagonist (1 μM)[3].

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

分子量

1018.08

Formula

C51H62F3N9O10

Sequence Shortening

Bz-AA-{D-Trp}-F-{D-Pro}-P-{Nle}-NH2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. A B McElroy, et al. Highly potent and selective heptapeptide antagonists of the neurokinin NK-2 receptor. J Med Chem. 1992 Jul 10;35(14):2582-91.

    [2]. M A Matuszek, et al. An investigation of tachykinin NK2 receptor subtypes in the rat. Eur J Pharmacol. 1998 Jul 3;352(1):103-9.

    [3]. Stephen D Tichenor, et al. Excitatory motor innervation in the canine rectoanal region: role of changing receptor populations. Br J Pharmacol. 2002 Dec;137(8):1321-9.

GR231118 TFA(Synonyms: 1229U91 TFA GW1229 TFA)

GR231118 TFA;(Synonyms: 1229U91 TFA; GW1229 TFA)

GR231118 是神经肽 Y 的 C 末端的类似物,对人神经肽 Y Y 受体具有较强的竞争性和相对选择性拮抗剂,其拮抗剂的 pKi 为10.4。GR231118 是人类神经肽 Y4 受体 (pEC50=8.6; pKi=9.6) 和对人及大鼠神经肽 YY2 和 Y5 受体的弱激动剂。GR231118 对小鼠神经肽 YY6 受体也有较高亲和力 (pKi= 8.8)。

GR231118 TFAamp;;(Synonyms: 1229U91 TFA; GW1229 TFA)

GR231118 TFA Chemical Structure

规格 是否有货
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250 mg ; 询价 ;
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生物活性

GR231118 TFA, an analogue of the C-terminus of neuropeptide Y, is a potent , competitive and relative seletive antagonist at human neuropeptide YY receptor with a pKi of 10.4. GR231118 a potent agonist at the human neuropeptide YY4 receptor (pEC50=8.6; pKi=9.6) and a weak agonist at the human and rat neuropeptide Y Y2 and Y5 receptors. GR231118 also has high affinity for the mouse neuropeptide YY6 receptor (pKi= 8.8)[1].

分子量

2466.76

Formula

C112H171F3N34O26

Sequence Shortening

Sequence 1:IEP-{Dpr}-YRLRY-NH2;Sequence 1′:IEP-{Dpr}-YRLRY-NH2 (Amide bridge:Glu2-Dpr4′;Dpr4-Glu2′)

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. E M Parker, et al. GR231118 (1229U91) and other analogues of the C-terminus of neuropeptide Y are potent neuropeptide Y Y1 receptor antagonists and neuropeptide Y Y4 receptor agonists. Eur J Pharmacol

    [2]. Y Dumont, et al. [(125)I]-GR231118: a high affinity radioligand to investigate neuropeptide Y Y(1) and Y(4) receptors. Br J Pharmacol. 2000 Jan;129(1):37-46.

GR-73632

GR-73632;

GR-73632 是新型速激肽神经激肽1 (NK-1) 受体激动剂。 GR-73632 通过传递瘙痒信号的 NK1 受体直接作用于初级感觉神经元的外周末端。

GR-73632amp;;

GR-73632 Chemical Structure

CAS No. : 133156-06-6

规格 是否有货
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生物活性

GR-73632 is a novel tachykinin neurokinin 1 (NK-1) receptor agonist[1]. GR-73632 acts directly on the peripheral terminals of primary sensory neurons through NK1 receptor which convey itch signals[2].

IC50 Target

IC50: NK-1 receptor[1]

分子量

766.00

Formula

C40H59N7O6S

CAS 号

133156-06-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Sakurada C, et al. Spinal actions of GR73632, a novel tachykinin NK1 receptor agonist. Peptides. 1999;20(2):301-4.

    [2]. Costantini VJ, et al. The NK1 receptor antagonist aprepitant attenuates NK1 agonist-induced scratching behaviour in the gerbil after intra-dermal, topical or oral administration. Exp Dermatol. 2015 Apr;24(4):312-4.

GR 64349

GR 64349;

GR 64349 是有效的、高度选择性的神经激肽 2 (NK2) 受体的肽类拮抗剂,其在大鼠结肠中测得的EC50 值为 3.7 nM。GR 64349 对 NK1 和NK3 受体的选择性要低1000 和 300 倍以上。

GR 64349amp;;

GR 64349 Chemical Structure

CAS No. : 137593-52-3

规格 是否有货
100 mg ; 询价 ;
250 mg ; 询价 ;
500 mg ; 询价 ;

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生物活性

GR 64349 is a potent and highly selective NK2 receptor peptide antagonist, with an EC50 of 3.7 nM in rat colon. GR 64349 exhibits selectivity >1000 and >300-fold with respect to NK1 and NK3 receptors, respectively[1][2].

分子量

921.11

Formula

C42H68N10O11S

CAS 号

137593-52-3

Sequence Shortening

KDSFV{Aaa}LM-NH2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Y Chang, et al. Tachykinin receptor subtypes in the isolated guinea pig heart and their role in mediating responses to neurokinin A. J Pharmacol Exp Ther. 2000 Jul;294(1):147-54.

    [2]. M J Deal, et al. Conformationally constrained tachykinin analogues: potent and highly selective neurokinin NK-2 receptor agonists. J Med Chem. 1992 Oct 30;35(22):4195-204.

GR 82334

GR 82334;

GR 82334 是一种有效的、特异性的可逆速激蛋白 NK1 受体 (tachykinin NK1 receptor) 拮抗剂。GR 82334 通过阻断 NK1 受体的作用,抑制大鼠神经肽 P 物质诱导的致敏作用。

GR 82334amp;;

GR 82334 Chemical Structure

CAS No. : 129623-01-4

规格 是否有货
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250 mg ; 询价 ;
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生物活性

GR 82334 is a potent and specific reversible tachykinin NK1 receptor antagonist[1]. GR 82334 inhibits substance P-induced sensitization by blocking SP NK1 receptors in naked mole-rats[1].

体内研究
(In Vivo)

GR 82334 (intrathecal administration; 0.1 nmol-1 nmol) excites rats unnary bladder motihty at 1 nmol but not at 0.1 nmol, and the reflex chemonociceptive is reduced by the topical application of capsaicin (4 μg/50 ul)[1].
GR 82334 (10 nM-1 µM; injected between vertebrae L4 and L5) has no effect at 10 nM in neither species, increases heat-induced foot withdrawal latency in mice at doses >100 nM, but no such increase in naked mole-rats, where doses >100 nM evoke a tendency for decreased latency[2].

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

Animal Model: 3-6 month-old, male C57BL/6 mice and 6-18 month-old naked mole-rats[2]
Dosage: 10 nM, 100 nM, and 1 µM
Administration: Lntrathecal injection between vertebrae L4 and L5 
Result: Increased heat-induced foot withdrawal latency in mice.

分子量

1386.55

Formula

C69H91N15O16

CAS 号

129623-01-4

Sequence Shortening

{Glp}ADPNKFY-{Aaa}-LW-NH2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. A Lecci,et al.Effect of the NK-1 receptor antagonist GR 82,334 on reflexly-induced bladder contractions. Life Sci

    [2]. Antje Brand, et al.  Functional neurokinin and NMDA receptor activity in an animal naturally lacking substance P: the naked mole-rat.PLoS One. 2010 Dec 21;5(12):e15162.

GR231118(Synonyms: 1229U91 GW1229)

GR231118;(Synonyms: 1229U91; GW1229)

GR231118 是神经肽Y 的 C 末端的类似物,对人神经肽 Y Y 受体具有较强的竞争性和相对选择性拮抗剂,其拮抗剂的 pKi 为10.4。GR231118 是人类神经肽 Y4 受体 (pEC50=8.6; pKi=9.6) 和对人及大鼠神经肽 YY2 和 Y5 受体的弱激动剂。GR231118 对小鼠神经肽 YY6 受体也有较高亲和力 (pKi= 8.8)。

GR231118amp;;(Synonyms: 1229U91;  GW1229)

GR231118 Chemical Structure

CAS No. : 158859-98-4

规格 是否有货
100 mg ; 询价 ;
250 mg ; 询价 ;
500 mg ; 询价 ;

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生物活性

GR231118, an analogue of the C-terminus of neuropeptide Y, is a potent , competitive and relative seletive antagonist at human neuropeptide Y Y receptor with a pKi of 10.4. GR231118 a potent agonist at the human neuropeptide Y Y4 receptor (pEC50=8.6; pKi=9.6) and a weak agonist at the human and rat neuropeptide YY2 and Y5 receptors. GR231118 also has high affinity for the mouse neuropeptide Y Y6 receptor (pKi= 8.8)[1].

分子量

2352.74

Formula

C110H170N34O24

CAS 号

158859-98-4

Sequence Shortening

Sequence 1:IEP-{Dpr}-YRLRY-NH2;Sequence 1′:IEP-{Dpr}-YRLRY-NH2 (Amide bridge:Glu2-Dpr4′;Dpr4-Glu2′)

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. E M Parker, et al. GR231118 (1229U91) and other analogues of the C-terminus of neuropeptide Y are potent neuropeptide Y Y1 receptor antagonists and neuropeptide Y Y4 receptor agonists. Eur J Pharmacol

    [2]. Y Dumont, et al. [(125)I]-GR231118: a high affinity radioligand to investigate neuropeptide Y Y(1) and Y(4) receptors. Br J Pharmacol. 2000 Jan;129(1):37-46.

GR 94800

GR 94800;

GR 94800 是有效的、选择性的神经激肽 2 (NK2) 受体的肽类拮抗剂,其对 NK2、NK1 和 NK3 受体的 pKB 值分别为 9.6、6.4 和 6.0。

GR 94800amp;;

GR 94800 Chemical Structure

CAS No. : 141636-65-9

规格 是否有货
100 mg ; 询价 ;
250 mg ; 询价 ;
500 mg ; 询价 ;

* Please select Quantity before adding items.

生物活性

GR 94800 is a potent and selective NK2 receptor peptide antagonist, with pKB values of 9.6, 6.4 and 6.0 for NK2, NK1 and NK3 receptors, respectively[1][2].

体外研究
(In Vitro)

Responses to EFS (15 Hz) were significantly reduced by the NK2 receptor antagonist GR 94800 (1 μM) either alone or in combination with the NK1 antagonist (1 μM)[3].

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

分子量

904.06

Formula

C49H61N9O8

CAS 号

141636-65-9

Sequence Shortening

Bz-AA-{D-Trp}-F-{D-Pro}-P-{Nle}-NH2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. A B McElroy, et al. Highly potent and selective heptapeptide antagonists of the neurokinin NK-2 receptor. J Med Chem. 1992 Jul 10;35(14):2582-91.

    [2]. M A Matuszek, et al. An investigation of tachykinin NK2 receptor subtypes in the rat. Eur J Pharmacol. 1998 Jul 3;352(1):103-9.

    [3]. Stephen D Tichenor, et al. Excitatory motor innervation in the canine rectoanal region: role of changing receptor populations. Br J Pharmacol. 2002 Dec;137(8):1321-9.