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21

抑制剂 & 化合物

11

天然产物

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Cat. No. Product Name Target Signaling Pathways
T9031 MCU-i4

Others; Mitochondrial Metabolism Metabolism; Others
MCU-i4 阻断IP3依赖的线粒体 Ca2+的摄取,是一种新型 MCU 负调节剂,可结合 MICU1 并损害肌肉细胞生长。
T23101 o-3M3FBS

Others Others
o-3M3FBS 是 m-3M3FBS 的阴性对照。它以独立于 PLC 的机制及拮抗方式抑制内向和外向电流。它以与 m-3M3FBS 竞争的方式增加 [Ca2+]i 增加。
TP1911L CALP3 acetate(261969-05-5 free base)

Calcium Channel Membrane transporter/Ion channel; Metabolism
CALP3 acetate(261969-05-5 free base) 是一种有效的 Ca2+ 通道阻滞剂,可激活 Ca2+ 结合蛋白的 EF 手基序。 它可以通过调节钙调蛋白 (CaM)、Ca2+ 通道和泵的活性在功能上模拟增加的 [Ca2+]i
T12201 Nebracetam hydrochloride

WEB 1881 FU hydrochloride

AChR Neuroscience
Nebracetam hydrochloride (WEB 1881 FU hydrochloride) 是促智 M1-毒蕈碱的激动剂。 它诱导细胞内 Ca2+ 浓度升高, EC50 为 1.59 mM。
T13904 18:0 LYSO-PE

Stearoyl lysophosphatidylethanolamine

Others Others
18:0 LYSO-PE是一种诱导[Ca2+]i增加的化合物,18:0 LYSO-PE可用作电喷雾质谱(ESI-MS)/MS进行脂质分析的磷脂(PL)标准。
TP1179L Porcine dynorphin A(1-13) acetate

Dynorphin A Porcine Fragment 1-13 acetate,Porcine dynorphin A(1-13) acetate(72957-38-1 free base)

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
Porcine dynorphin A(1-13) acetate (Dynorphin A Porcine Fragment 1-13 acetate)(72957-38-1 free base) 是一种有效的内源性 κ opioid 受体激动剂,在生理浓度下具有镇痛作用。暴露于强啡肽 A (1-13) 会导致单个神经元中 [Ca2+]i 的急剧增加,类似于急性 NMDA 治疗所见的增加。
TP2170 CALP3 TFA(261969-05-5 free base)

CALP3 TFA

Calcium Channel Membrane transporter/Ion channel; Metabolism
CALP3 TFA is a potent Ca2+ channel blocker that activates EF-hand motifs of Ca2+-binding proteins. It can functionally mimic increased [Ca2+]i by modulating the activity of Calmodulin, Ca2+ channels, and pumps.
T75789 CALP3 TFA

CALP3 TFA 是一种模拟 Ca2+ 的有效肽类 Ca2+ 通道阻断剂,能够激活 EF 手的 Ca2+ 结合蛋白。它通过影响钙调蛋白 (CaM)、Ca2+ 通道及泵的功能来模拟 [Ca2+]i 的增加,从而具备在控制 HIV 或缺血性神经元损伤等情况下调控细胞凋亡的能力。
T75928 des-​Gln14-​Ghrelin TFA

des-Gln14-Ghrelin TFA为生长激素促分泌受体的第二个内源性配体。该化合物能在CHO-GHSR62细胞中诱导[Ca2+]I的提升,其EC50值为2.4 nM。
T69357 AL-34662

AL-34662 is a serotonin-2 receptor agonist with antihypertensive action. AL-34662 has a high-affinity for the 5-HT2 receptor and may potentially lead mobilization of [Ca2+]i in h-CM and h-TM cells leading to a decrease in ocular pressure.
TP1179 Porcine dynorphin A(1-13)

Dynorphin A Porcine Fragment 1-13

Porcine dynorphin A (1-13) is a potent, endogenous κ opioid receptor agonist and is antinociceptive at physiological concentrations. Exposure to dynorphin A (1-13) causes acute increases in [Ca2+]i in individual neurons similar to increases seen with acut
TP1532 γ-2-MSH (41-58), amide

Melanocortin (MC) 3-MSH (Melanocyte-Stimulating Hormone) is believed to signal through the MC 3 receptor. It induces a sustained increase in intracellular free calcium levels ([Ca2+]i) in a subpopulation of pituitary cells. Most of the cells responding to
T41204 TAT-Gap19(I130A)

TAT-Gap19(I130A)

TAT-Gap19(I130A) is a control peptide for TAT-Gap19, a Cx43 hemichannel blocker. TAT-Gap19(I130A) consists of TAT-GAP19 with a I130A amino acid residue change at a key residue for GAP19 activity. In C6 glioma cells expression Cx43, TAT-GAP19(1130A) does not inhibit [Ca2+]i-triggered ATP release at 200 μM. TAT-Gap19(I130A) is cell permeable.
T80191 His-D-beta-Nal-Ala-Trp-D-Phe-Lys-NH2 TFA

Endogenous Metabolite Metabolism
His-D-beta-Nal-Ala-Trp-D-Phe-Lys-NH2 TFA,GHRP-1的一种代谢产物,属于生长激素释放肽类。作为Ala-His-D-beta-Nal-Ala-Trp-D-Phe-Lys-NH2的同义物,GHRP-1能够刺激GH(生长激素)的释放。在大鼠垂体静态单层细胞试验中,GHRP-1可提高GH释放率和[Ca2+]i水平,但对cAMP浓度无显著影响。
T62243 Bepridil hydrochloride hydrate

Bepridil hydrochloride hydrate ((±)-Bepridil hydrochloride hydrate) 是一种长效的、非选择性的钙离子通道 (Ca+channel) 拮抗剂。Bepridil hydrochloride hydrate 是一种钠离子、钾离子通道 (Na+,K+channel) 抑制剂,也是心脏 Na+/Ca2+交换 (NCX1) 抑制剂。Bepridil hydrochloride hydrate 具有抗心绞痛和抗 I 型心律失常作用,能够用于研究心血管疾病。
T75936 RVD-Hpα TFA

RVD-Hpα TFA is the N-terminally extended form of human hemopressin that acts as a selectiveCB1receptoragonist. RVD-Hpα TFA increases intracellular Ca2+levels in cells expressingCB1receptors in vitro. RVD-Hpα TFA also high affinityCB2positive allosteric modulator (Ki=50 nM).
T69206 AL-38022A

AL-38022A is a novel synthetic serotonergic (5-HT) ligand that exhibited high affinity for each of the 5-HT2 receptor subtypes (Ki<or=2.2 nM), but a significantly lower (>100-fold less) affinity for other 5-HT receptors. In addition, AL-38022A displayed a very low affinity for a broad array of other receptors, neurotransmitter transport sites, ion channels, and second messenger elements, making it a relatively selective agent. AL-38022A potently stimulated functional responses via native and clo...
T35459 Glycyl H-1152 hydrochloride

Two Rho-associated kinases (ROCK), ROCK-I and ROCK-II, act downstream of the G protein Rho to regulate cytoskeletal stability. The ROCKs play important roles in diverse cellular functions including cell adhesion and proliferation, smooth muscle contraction, and stem cell renewal. Glycyl-H-1152 is a selective and potent ROCK inhibitor (IC50 = 11.8 nM for ROCK-II). It is a glycylated isoquinoline compound derived from the therapeutically-important ROCK inhibitor HA-1077 (Fasudil) and exhibits bett...
T76021 Myelin Basic Protein TFA

Myelin Basic Protein (MHP4-14) TFA 是一种合成肽,包含髓鞘碱性蛋白的残基4-14,是一种非常有选择性的 PKC 底物 (Km=7 μM)。Myelin Basic Protein TFA 不被环腺苷酸依赖性蛋白激酶、酪蛋白激酶 IIICa2+/钙调素依赖性蛋白激酶 II 或磷酸化酶激酶磷酸化,可常规用于测定粗组织提取物中低背景的蛋白激酶 C。
T73453 MRS4719

MRS4719 是一种有效的P2X4受体拮抗剂,对人 P2X4 受体的IC50为 0.503 μM。MRS4719 可减少脑梗死体积,减少脑萎缩,在缺血性脑中风模型中具有神经保护和神经康复作用。MRS4719 还能减少 ATP 诱导的人单核细胞源性巨噬细胞 [Ca2+]i 内流。MRS4719 可用于研究缺血性脑中风。
T36007 Nebentan

Nebentan (YM598) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan . Nebentan inhibits [125I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with Ki of 0.697 nM and 569 nM, respectively[1]. YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo[2]. Nebentan inhibits the specific binding of [125I] endothelin-1 to endothelin ETA and ETB receptors in a concentration dep...

化合物

MCU-i4
Cat.No: T9031
Synonym:
Target: Others, Mitochondrial Metabolism
o-3M3FBS
Cat.No: T23101
Synonym:
Target: Others
CALP3 acetate(261969-05-5 free base)
Cat.No: TP1911L
Synonym:
Target: Calcium Channel
Nebracetam hydrochloride
Cat.No: T12201
Synonym: WEB 1881 FU hydrochloride
Target: AChR
18:0 LYSO-PE
Cat.No: T13904
Synonym: Stearoyl lysophosphatidylethanolamine
Target: Others
Porcine dynorphin A(1-13) acetate
Cat.No: TP1179L
Synonym: Dynorphin A Porcine Fragment 1-13 acetate,Porcine dynorphin A(1-13) acetate(72957-38-1 free base)
Target: Opioid Receptor
CALP3 TFA(261969-05-5 free base)
Cat.No: TP2170
Synonym: CALP3 TFA
Target: Calcium Channel
CALP3 TFA
Cat.No: T75789
Synonym:
Target:
des-​Gln14-​Ghrelin TFA
Cat.No: T75928
Synonym:
Target:
AL-34662
Cat.No: T69357
Synonym:
Target:
Porcine dynorphin A(1-13)
Cat.No: TP1179
Synonym: Dynorphin A Porcine Fragment 1-13
Target:
γ-2-MSH (41-58), amide
Cat.No: TP1532
Synonym:
Target:
TAT-Gap19(I130A)
Cat.No: T41204
Synonym: TAT-Gap19(I130A)
Target:
His-D-beta-Nal-Ala-Trp-D-Phe-Lys-NH2 TFA
Cat.No: T80191
Synonym:
Target: Endogenous Metabolite
Bepridil hydrochloride hydrate
Cat.No: T62243
Synonym:
Target:
RVD-Hpα TFA
Cat.No: T75936
Synonym:
Target:
AL-38022A
Cat.No: T69206
Synonym:
Target:
Glycyl H-1152 hydrochloride
Cat.No: T35459
Synonym:
Target:
Myelin Basic Protein TFA
Cat.No: T76021
Synonym:
Target:
MRS4719
Cat.No: T73453
Synonym:
Target:
Nebentan
Cat.No: T36007
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T6856 Halofuginone

卤夫酮,常山酮,Tempostatin,empostatin,RU-19110

Calcium Channel; DNA/RNA Synthesis; Sodium Channel; Parasite; TGF-beta/Smad Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Membrane transporter/Ion channel; Metabolism; Microbiology/Virology; Stem Cells
Halofuginone (RU-19110) 是Febrifugine 的衍生物,是一种竞争性脯氨酰-tRNA 合成酶抑制剂。它也是肺血管扩张剂,可激活Kv 通道并阻断电压门控、受体操作和存储操作的钙离子通道。它具有抗炎、抗癌、抗疟疾和抗纤维化作用。
T3524 Halofuginone hydrobromide

卤夫酮溴氢酸盐,Tempostatin,RU-19110 (hydrobromide),Stenorol,常山酮溴酸盐

Others; Calcium Channel; DNA/RNA Synthesis; Sodium Channel; Parasite; TGF-beta/Smad Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Membrane transporter/Ion channel; Metabolism; Microbiology/Virology; Others; Stem Cells
Halofuginone hydrobromid 是Febrifugine 的衍生物,是竞争性脯氨酰-tRNA 合成酶抑制剂。它是 I 型胶原合成的特异性抑制剂,并通过抑制TGF-β活性可减轻骨关节炎。它具有抗疟疾、抗炎、抗癌、抗纤维化作用。
TN2322 Yangambin

Calcium Channel; PAFR GPCR/G Protein; Membrane transporter/Ion channel; Metabolism
Yangambin 是从诸如番荔枝科植物中分离出来的呋喃木脂素,是选择性PAF 受体拮抗剂,通过调控Ca2+通道抑制 Ca2+流入,导致 [Ca2+]i 在血管平滑肌细胞和随后的外周血管舒张中减少,具有降压作用。
T5S0527 Rhodojaponin III

闹羊花素 Ⅲ,闹羊花毒素III

Others Others
Rhodojaponin III 是二萜类化合物,提取于Rhododendron molle 叶子,具有抗炎作用。
T5S1632 Barlerin

8-O-乙酰山栀苷甲酯,8-O-Acetylshanzhiside methyl ester,ND01

VEGFR; TNF; NF-κB; Akt; Caspase Angiogenesis; Apoptosis; Cytoskeletal Signaling; NF-κB; PI3K/Akt/mTOR signaling; Proteases/Proteasome; Tyrosine Kinase/Adaptors
Barlerin (8-O-Acetylshanzhiside methyl ester) 是一种环孢菌素葡萄糖苷,从中国西藏民间药用植物中分离得到,能够抑制NF-κB 活性。
T1407 (-)-Menthol

L-Menthol,Levomenthol,(-)-薄荷醇,薄荷冰,Menthomenthol,Menthacamphor

Opioid Receptor; Endogenous Metabolite; TRP/TRPV Channel Endocrinology/Hormones; GPCR/G Protein; Membrane transporter/Ion channel; Metabolism; Neuroscience
(-)-Menthol (Levomenthol) 分离自薄荷油,L-Menthol 是瞬时受体电位 M8 (TRPM8)的激活剂,TRPM8 是 Ca2+-可渗透的非选择性阳离子通道,并增加 [Ca2+]i。L-Menthol 具有抗肿瘤活性。
T6S1418 Praeruptorin C

Antioxidant; Calcium Channel Membrane transporter/Ion channel; Metabolism; oxidation-reduction
Praeruptorin C 是白花前胡中的一种主要成分,是钙拮抗剂,pD2′值为 5.7。
T7009 Soyacerebroside II

IL Receptor; Calcium Channel Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism
Soyacerebroside II exhibits ionophoretic activity for Ca2+ ion. Soyacerebrosides I and II have modulating the cellular immune response effects, they show obvious inhibitory activity on IL-18 secretion in human peripheral blood mononuclear cells (PBMC).
TN2169 Saikogenin D

柴胡皂甙元 D,皂苷元 D

IL Receptor; Calcium Channel; Prostaglandin Receptor GPCR/G Protein; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism
Saikogenin D possesses a dual effect: an inhibition of A23187-induced PGE2 production without a direct inhibition of cyclooxygenase activity; and an elevation of [Ca2+]i that is attributed to Ca2+ release from intracellular stores. Saikogenin D has immuno
TN3660 Cinnamyl caffeate

Calcium Channel Membrane transporter/Ion channel; Metabolism
Cinnamyl caffeate has cardiovascular protective effects, it can increase H9c2 cellular antioxidant potential, decrease intracellular calcium ion ([Ca2+]i) level, and prevent cell apoptosis; it possesses potent antiproliferative activity with the EC(50) value of 0.114 microM, toward colon 26-L5 carcinoma. Cinnamyl caffeate possesses potent NO inhibitory activity with the IC(50) value of 9.53 microM.
TN2641 15-Methoxypinusolidic acid

ERK; IL Receptor; p38 MAPK; Calcium Channel; NOS; NF-κB; COX; JNK; NMDAR; PPAR DNA Damage/DNA Repair; Immunology/Inflammation; MAPK; Membrane transporter/Ion channel; Metabolism; Neuroscience; NF-κB
15-Methoxypinusolidic acid has anti-inflammatory effects, it inhibits LPS-induced iNOS expression and NO production, independent on MAPK and NF-kappaB. 15-Methoxypinusolidic acid suppresses adipocyte differentiation through the inhibition of PPARgamma-dep

天然产物

Halofuginone
Cat.No: T6856
Synonym: 卤夫酮,常山酮,Tempostatin,empostatin,RU-19110
Target: Calcium Channel, DNA/RNA Synthesis, Sodium Channel, Parasite, TGF-beta/Smad
Halofuginone hydrobromide
Cat.No: T3524
Synonym: 卤夫酮溴氢酸盐,Tempostatin,RU-19110 (hydrobromide),Stenorol,常山酮溴酸盐
Target: Others, Calcium Channel, DNA/RNA Synthesis, Sodium Channel, Parasite, TGF-beta/Smad
Yangambin
Cat.No: TN2322
Synonym:
Target: Calcium Channel, PAFR
Rhodojaponin III
Cat.No: T5S0527
Synonym: 闹羊花素 Ⅲ,闹羊花毒素III
Target: Others
Barlerin
Cat.No: T5S1632
Synonym: 8-O-乙酰山栀苷甲酯,8-O-Acetylshanzhiside methyl ester,ND01
Target: VEGFR, TNF, NF-κB, Akt, Caspase
(-)-Menthol
Cat.No: T1407
Synonym: L-Menthol,Levomenthol,(-)-薄荷醇,薄荷冰,Menthomenthol,Menthacamphor
Target: Opioid Receptor, Endogenous Metabolite, TRP/TRPV Channel
Praeruptorin C
Cat.No: T6S1418
Synonym:
Target: Antioxidant, Calcium Channel
Soyacerebroside II
Cat.No: T7009
Synonym:
Target: IL Receptor, Calcium Channel
Saikogenin D
Cat.No: TN2169
Synonym: 柴胡皂甙元 D,皂苷元 D
Target: IL Receptor, Calcium Channel, Prostaglandin Receptor
Cinnamyl caffeate
Cat.No: TN3660
Synonym:
Target: Calcium Channel
15-Methoxypinusolidic acid
Cat.No: TN2641
Synonym:
Target: ERK, IL Receptor, p38 MAPK, Calcium Channel, NOS, NF-κB, COX, JNK, NMDAR, PPAR
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