标签归档：gr

GR 64349 TFA

发表于由

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
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

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

发表于由

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
100 mg ; 询价 ;
250 mg ; 询价 ;
500 mg ; 询价 ;

* Please select Quantity before adding items.

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)

发表于由

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
100 mg ; 询价 ;
250 mg ; 询价 ;
500 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

发表于由

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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250 mg ; 询价 ;
500 mg ; 询价 ;

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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

发表于由

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 ;

* Please select Quantity before adding items.

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

发表于由

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 ;
500 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)

发表于由

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 ;

* Please select Quantity before adding items.

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

发表于由

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.

新型的调控植物株型的激素—独角金内酯类似物GR24

发表于由

独角金内酯是一些天然的独角金醇类化合物及人工合成类似物的总称，是新型调控植物株型的重要激素。GR24是一类以独角金内酯为基础的人工合成的化学物质，其中rac-GR24（CAS号：76974-79-3，分子式C17H14O5）是独角金内酯类似物中最有效的一个。


新型的调控植物株型的激素—独角金内酯类似物GR24

上海金畔生物科技有限公司独家提供多种独角金内酯类似物：

货号

品名

规格

G3324

（+/-）-GR24

1 – 5 mg

G24

GR24rac

1 – 500 mg

EN1

GR24 5DS

5 – 100 mg

EN2

GR24 ent-5DS

5 – 100 mg

EN3

GR24 ent-4DO

5 – 100 mg

EN4

GR24 4DO

5 – 100 mg

GBI

Biotin-labelled-GR24

5 – 50 mg

GBO

GR24-BODIPY

0.5 – 2 mg


独角金内酯在杂草检验检疫、杂草控制、植株塑型等方面都有着重要的应用价值和科研价值。

独角金内酯的生物活性：

1、调节植物与丛枝菌根真菌的共生关系 研究发现，独角金内酯能够促进丛枝菌根真菌菌丝分支，以此和植物建立共生关系。植物能够为丛枝菌根真菌提供有机物，维持其生长需要，另一方面，丛枝菌根真菌从土壤中吸收寄主所需要的养分来，用于氨基酸的合成，帮助植物吸收水分和营养物质，提高植物对于来自生物的或者非生物胁迫的抗性。

2、刺激寄生植物种子萌发，防治寄生杂草 独角金内酯从植物的根中释放，可诱导根寄生杂草如独角金属、列当属的种子萌发。根寄生植物对农作物有很大的破坏性，能通过寄生在植物的根部，掠夺植物的营养和水分。寄生植物的种子都非常小，贮藏的营养有限，它们一旦萌发就必须在几天之内接触到寄主并寄生其上，否则就会死去，利用此原理，可以开发天然或人工合成的萌发刺激物，诱导寄生植物种子进行“自杀”，可作为根寄生杂草防治的一条新路径。

3、抑制植物的分枝，调控植物株型 据研究显示，独角金内酯及其类似物能够抑制植物芽的分枝。可以利用这一特点来控制农作物的分枝，提高水稻、大豆等粮食作物产量，也可以促进果树分枝，达到高产的效果。