Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T2584 |
Octreotide
SMS 201-995,奥曲肽 |
Somatostatin | GPCR/G Protein |
Octreotide (SMS 201-995) 是一种有效的生长激素、胰高血糖素和胰岛素抑制剂。它主要与生长抑素 2、3 和 5 亚型受体结合,可增强 Gi 活性,降低胞内 cAMP 的产生。 | |||
TP2207 |
Pasireotide Acetate
|
Somatostatin | GPCR/G Protein |
Pasireotide acetate 是长效的环己肽生长激素抑制素类似物,具有抗分泌、抗增殖和促凋亡活性。它可抑制 GH、IGF-I 和 ACTH 的分泌,可用于研究肢端肥大症和库欣病。它还可以提高生长抑素受体的激动剂活性,对sst1、2、3、4、5的pKi 分别为 8.2、9.0、9.1、小于7.0 和 9.9。 | |||
T9692 |
Paltusotine
|
Somatostatin | GPCR/G Protein |
Paltusotine 是一种口服有效的,非肽选择性生长抑素 2 型受体激动剂。在长效生长抑素受体配体作用后,Paltusotine 仍可维持 GH 和 IGF-1 水平。 | |||
T4119 |
Octreotide Acetate
醋酸奥曲肽,SMS 201995,Longastatin,Sandostatin,SMS 201-995 (acetate) |
Somatostatin | GPCR/G Protein |
Octreotide Acetate (Sandostatin) 是一种长期有效的合成生长抑素八肽类似物,可抑制生长激素的分泌。 | |||
TP2045 |
CH 275
|
||
Potent somatostatin receptor 1 (sst1) agonist; displays selectivity for sst1 (IC50 values are 30.9 nM, 345 nM, > 1 μM, > 10 μM and > 10μM for human sst1, sst3, sst4, sst2 and sst5 respectively). Attenuates somatostatin release in the rat nucleus accumbens | |||
TP2052L |
CTOP acetate
|
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
CTOP acetate 是一种生长抑素类似物和μ-阿片受体拮抗剂。 | |||
T28743 |
Seglitide acetate
MK 678,MK678,MK-678 |
Somatostatin | GPCR/G Protein |
Seglitide acetate (MK-678) 是一种选择性的 sst2生长抑素受体激动剂。 | |||
TP1346 |
CYN 154806 TFA
CYN 154806 TFA |
Somatostatin | GPCR/G Protein |
CYN 154806 TFA(183658-72-2 free base) 是一种环状八肽,是一种有效的选择性生长抑素 sst2 受体拮抗剂。对于重组 sst2、sst1、sst3、sst4 和 sst5 受体,pIC50 值分别为 8.58、5.41、6.07、5.76 和 6.48。 | |||
T27787L |
L-797,591 hydrochloride
L-797,591 hydrochloride(217480-24-5 Free base) |
||
L-797,591 hydrochloride 对生长抑素受体亚型 1 (SSTR1)有活性。L-797,591 hydrochloride 常与 AG1478 联合使用来增强表达 SSTR1的细胞中 p-ERK5的表达。L-797,591 hydrochloride 在共转染的细胞中显著增强了 p38的磷酸化,这一作用在与 AG1478联合处理时被逆转。 | |||
TP2050L |
CTAP(TFA) (103429-32-9 free base)
CTAP(TFA) |
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
CTAP(TFA) (103429-32-9 free base) 是一种有效的、高度选择性的、脑渗透性 μ-阿片受体拮抗剂,IC50 为 3.5 nM。它的选择性比 δ 阿片类药物 (IC50=4500 nM) 和生长抑素受体高 1200 倍以上。 CTAP TFA 可用于研究 L-DOPA 诱导的运动障碍 (LID) | |||
T23073 |
NNC 26-9100
|
Others | Others |
Somatostatin sst4 receptor agonist | |||
T24860 |
TC-G1003
TC G1003 |
||
TC-G1003 is an effective agonist of the somatostatin sst2 receptor. | |||
T28220 |
NVP ACQ090
NVP-ACQ090,ACQ090,ACQ 090,NVPACQ090,ACQ-090 |
||
NVP ACQ090 is a potent and subtype-selective somatostatin sst(3) receptor antagonist. | |||
T69836 | Paltusotine HCl | ||
Paltusotine, also known as CRN00808, is a somatostatin receptor agonist. | |||
TP1810 |
Somatostatin-25
|
||
Somatostatin is an endogenous neuropeptide hormone found in the brain and pancreas. Somatostatin binds several isoforms of the somatostatin receptor, exhibiting anxiolytic, antiepileptic/anticonvulsant, and anorexigenic activities. | |||
T27783 |
L-779976
L-779,976,L779,976,L779976,L 779976,L 779,976 |
||
L-779,976 is an agonist of somatostatin receptor. | |||
T22487 | (1R,1'S,3'R/1R,1'R,3'S)-L-054,264 | Others | Others |
somatostatin sst2 receptor agonist | |||
T31606 |
EE 581
EE581,EE-581 |
||
EE 581 can be used to label the somatostatin receptor. | |||
T34592 |
Sdz 215-811
Sdz-215-811,Pentatreotide,Sdz215-811,Octreoscan 111 |
||
Sdz 215-811 is a potential radiopharmaceutical used in somatostatin receptor-positive tumors imaging. | |||
T22907 |
L-817,818
|
Others | Others |
somatostatin sst5 receptor agonist | |||
T27787 |
L-797,591
|
||
L-797,591 is a selective agonist of somatostatin receptor subtype 1. | |||
T28298 |
Pasireotide diaspartate
SOM-230,SOM230,trade name: Signifor,SOM 230,Signifor LAR |
||
Pasireotide is a somatostatin analog with a 40-fold increased affinity to somatostatin receptor 5 compared to other somatostatin analogs. | |||
T16469 |
Pentetreotide
|
Others | Others |
Pentetreotide is an indium-labeled somatostatin analog and can be used for nuclear medicine imaging. Pentetreotide is a diethylenetriaminopentaacetic conjugate of Octreotide. Somatostatin receptor scintigraphy with Pentetreotide is effective in visualizin | |||
T27761 |
L-054,522
L054,522 |
||
L-054,522 is potent, selective agonists of somatostatin receptor. | |||
T13022 | SSTR5 antagonist 2 | Others | Others |
SSTR5 antagonist 2 is a highly potent, oral active and selective antagonist of somatostatin (receptor) subtype 5 (SSTR5),with potential to treat type 2 diabetes mellitus (T2DM). | |||
T13306L2 | Vapreotide diacetate | ||
Vapreotide diacetate is a synthetic analog of somatostatin. It has analgesic activity most likely mediated through the blockade of the neurokinin-1 receptor (NK1R), the substance P (SP)-preferring receptor. | |||
T76596 |
PRL 3195
|
||
PRL 3195 是一种somatostatin receptor 拮抗剂,对人生长抑素受体 sst5、sst2、sst3、sst1和 sst4的Ki 分别为 6、17、66、1000 和 1000 nM。 | |||
T26225 |
SRA880 malonate
SRA880,NVPSRA880,NVP-SRA880,NVP-SRA-880,NVP-SRA 880,NVP SRA880 |
||
SRA880 is a non-peptide somatostatin sst(1) receptor antagonist which displays a significantly lower affinity for the other human recombinant somatostatin receptors ( pK(d)= 6.0) or a wide range of neurotransmitter receptors, except for the human dopamine | |||
T13022L |
SSTR5 antagonist 2 TFA
|
Others | Others |
SSTR5 antagonist 2 TFA is a highly potent, oral active and selective antagonist of somatostatin (receptor) subtype 5 (SSTR5), with potential to treat type 2 diabetes mellitus (T2DM). | |||
T28851 |
SRA880 free base
SRA 880,NVPSRA880,NVP SRA880,NVP-SRA880,SRA-880,SRA880 |
||
SRA880 is a non-peptide antagonist of somatostatin sst1-receptor. SRA880 displayed significantly lower affinity for the other human recombinant somatostatin receptors ( pK(d) < or = 6.0). SRA880 shows a certain binding affinity to the human dopamine D4 re | |||
T13005 | SSTR5 antagonist 1 | Others | Others |
SSTR5 antagonist 1 is a selective, and orally available antagonist of somatostatin receptor subtype 5 (SSTR5)(IC50s of 9.6 and 57 nM for hSSTR5 and mSSTR5, respectively). | |||
T39207 |
L-803087 TFA
|
||
L-803087 TFA is a highly potent and selective agonist of the somatostatin sst4 receptor, exhibiting a Ki value of 0.7 nM. It displays a remarkable selectivity, being over 280-fold more preferential for the sst4 receptor compared to other somatostatin receptors. Furthermore, L-803087 TFA promotes AMPA-mediated synaptic responses in hippocampal preparations and enhances kainate-induced seizures in mice. | |||
TP2124 |
Somatostatin 1-28
|
||
Somatostatin receptor agonist, derived from the post-translational cleavage of prosomatostatin. | |||
T75842 |
Cyclosomatostatin TFA
|
||
Cyclosomatostatin TFA 作为一种有效的生长抑素(SST)受体拮抗剂,在直肠癌(CRC)细胞中通过抑制1型生长抑素受体(SSTR1)的信号传导,有效降低结细胞增殖、ALDH+细胞群体的大小以及球形成。 | |||
T76544 |
Cyclic SSTR agonist octreotide
|
||
Cyclic SSTR agonist octreotide 是一种 Octreotide ,可作为生长抑素受体 (SSTR) 的激动剂。 | |||
TP2050 |
CTAP
|
||
Potent and selective μ opioid receptor antagonist (IC50 = 3.5 nM). Displays > 1200-fold selectivity over δ opioid and somatostatin receptors. Brain penetrant and active in vivo. | |||
TP1877 |
CYN 154806
|
||
CYN 154806 is a potent and selective somatostatin sst2 receptor antagonist, The pIC50 values are 8.58, 5.41, 6.07, 5.76 and 6.48 for human recombinant sst2, sst1, sst3, sst4 and sst5 receptors respectively. | |||
TP2420 |
Veldoreotide
DG 3173,DG3173,PTR 3173,DG-3173,Somatoprim |
||
Veldoreotide, also known as Somatoprim, is a unique somatostatin receptor subtypes 2-, 4- and 5-selective analogue which effectively reduces GH secretion in human GH-secreting pituitary adenomas, even in Octreotide non-responsive tumours. | |||
T32511L |
L-796,778 acetate
L-796,778 acetate(217480-25-6 Free base) |
Somatostatin | GPCR/G Protein |
L-796,778 acetate 是一种选择性生长抑素受体激动剂,对 sst3的IC50为24nM,对sst1、sst2、sst4和sst5的IC50大于1000nM。 | |||
T11700 |
J-2156
|
Others | Others |
The ED50 of J-2156 in rats for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws was 3.7 and 8.0 mg/kg, respectively. J-2156 is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC5 | |||
TP1804 |
PEN-221
|
||
PEN-221 is a Somatostatin receptor 2 (SSTR2)-targeting cytotoxic conjugate with an IC50 of 10 nM. PEN-221 is a conjugate consisting of microtubule-targeting agent DM1 linked to the C-terminal side chain of Tyr3-octreotate. | |||
T76594 |
PRL 2915
|
||
PRL 2915 是一种有效的人类生长抑素亚型 2 受体拮抗剂 (hsst2),其Ki 为 12 nM。 | |||
T75248 | Pasireotide (diaspartate) | ||
Pasireotide (SOM230) diaspartate 是一种长效的环己肽生长激素抑制素类似物,可以提高生长抑素受体的激动剂活性,对sst1/2/3/4/5的pKi 分别为 8.2/9.0/9.1/<7.0/9.9。Pasireotide diaspartate 具有抗分泌、抗增殖和促凋亡活性。 | |||
T82883 |
BIM-23027
|
||
BIM-23027为高选择性sst2受体激动剂(EC50=0.32 nM),其功能效果类似生长抑素(SRIF,环状十四肽)。该化合物可促进多巴胺的释放,此过程通过Glu依赖的机制进行调控。 | |||
T80157 |
DOTA-JR11
|
||
DOTA-JR11为SSTR2生长抑素受体拮抗剂,能经68Ga标记,应用于神经内分泌肿瘤(NETs)配对成像研究。 | |||
T75917 |
CTAP TFA
|
||
CTAP TFA 是一种强效、高选择性的、可透过血脑屏障的阿片受体 (μopioid receptor) 拮抗剂,IC50为 3.5 nM。CTAP TFA 对δ opioid 受体 (IC50=4500 nM) 和生长抑素受体 (somatostatin receptors) 具有超过 1200 倍的选择性。CTAP TFA 可用于L -多巴胺 诱导的运动障碍 (LID) 和阿片类活性分子过量或成瘾的研究。 | |||
T60784 |
SSTR4 agonist 2
|
||
SSTR4 agonist 2 是有效的生长抑素受体亚型 4 (SSTR4) 激动剂,在 SSTR4 相关的医学疾病研究中具有潜力。SSTR4 通路抑制痛觉和炎症。 | |||
T76331 |
Cortistatin 29
|
||
Cortistatin 29,一种具备高亲和力结合至所有生长抑素(SS)受体亚型的神经肽,其对SSTR1、SSTR2、SSTR3、SSTR4、SSTR5的IC50值分别为2.8, 7.1, 0.2, 3.0, 13.7 nM。该化合物不仅能减轻神经性疼痛,还表现出抗纤维化作用。 | |||
T81571 |
PACAP (1-38) free acid TFA
|
||
PACAP (1-38) free acid TFA,一种内源性神经肽,能有效促进胃窦运动,增强体液蛋白分泌,同时抑制胃泌素释放。此外,它刺激血管活性肠肽、胃泌素释放肽和P物质的释放,并通过RACK1增强N-甲基-D-天门冬氨酸受体功能及脑源性神经营养因子表达。 | |||
T76980 | Tidutamab | ||
Tidutamab (XmAb-18087) 是一种具有完整 Fc 结构域的人源化及亲和优化双特异性抗体(bsAb),旨在通过SSTR2和CD3两个靶点特异性结合来延长血清半衰期,通过激活T细胞介导的细胞毒性(RTcC)机制,有效消除SSTR+肿瘤细胞。 |