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33

抑制剂 & 化合物

1

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T83174	Activated EG3 Tail
	Activated EG3 Tail 适用于合成外显子跳跃寡聚物偶联物。该寡聚物偶联物能与人类抗肌萎缩蛋白基因特定的靶位点匹配，进而诱导外显子 51 的跳跃。此类偶联物对于肌肉萎缩症研究具有重要价值。
T77267	C13-113-tri-tail
	C13-113-tri tail 是一种阳离子类脂化合物，可用于配制脂质纳米颗粒。
T77268	C13-112-tetra-tail
	C13-112-tetra-tail 是一种阳离子类脂化合物，可用于配制脂质纳米颗粒。
T77266	C13-112-tri-tail
	C13-112-tri-tail 是一种阳离子类脂化合物，可用于配制脂质纳米颗粒。
T77269	C13-113-tetra-tail
	C13-113-tetra-tail 是一种阳离子类脂化合物，可用于配制脂质纳米颗粒。
T1496	Amiodarone hydrochloride 盐酸胺碘酮,Amiodar,Amiodarone HCl,Nexterone	Potassium Channel; Adrenergic Receptor; Autophagy	Autophagy; GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience
	Amiodarone hydrochloride (Amiodarone HCl) 是一种抗心绞痛和 III 类抗心律失常药物，通过抑制钾通道和电压门控钠通道来增加心室和心房肌肉作用的持续时间，可导致心率和血管阻力降低。它通过成纤维细胞中的 ERK1/2和 p38 MAPK 信号传导诱导细胞增殖和肌成纤维细胞分化，可研究室上性和室性心律失常。
T2141	Mecamylamine hydrochloride 盐酸美加明,Inversine,Mevasin	AChR	Neuroscience
	Mecamylamine hydrochloride (Mevasin) 是一种易穿过血脑屏障的烟碱拮抗剂，用作高血压的神经节阻滞剂，具有抗神经疾病作用。
T1909	L-701324 7-氯-4-羟基-3-(3-苯氧基)苯基-2(1H)-喹啉,L701324	NMDAR; iGluR	Membrane transporter/Ion channel; Neuroscience
	L-701324 是一种 NMDA 受体，对甘氨酸位点具有高亲和力和选择性，用作口服活性和长效抗惊厥药。
T10337	Antimicrobial Compound 1	Antibacterial	Microbiology/Virology
	Antimicrobial Compound 1 是一种烷基吡啶鎓化合物，尾部为 12C，头部为 4-羧基。 Antimicrobial Compound 1 对枯草芽孢杆菌和大肠杆菌具有抗菌活性。
T3157	COH29 RNR Inhibitor COH29	DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	COH29 (RNR Inhibitor COH29) 是一种口服可用的芳香族取代噻唑，是人类核糖核苷酸还原酶 (RNR) 的抑制剂，具有潜在的抗肿瘤活性。它抑制核糖核苷酸还原酶的IC50为 16 μM。
T31475	Dihydropteroyl hexaglutamate
	Dihydropteroyl hexaglutamate is a link binding together sub-structures of the tail of Escherichia coli bacteriophage T4.
T38210	Hodgkinsine B
	Hodgkinsine B is an alkaloid and isomer of hodgkinsine that has analgesic activity.1It increases the latency to tail withdrawal in the tail-flick test in mice when administered at a dose of 10 mg/kg. 1.Kodanko, J.J., Hiebert, S., Peterson, E.A., et al.Synthesis of all low-energy stereoisomers of the tris(pyrrolidinoindoline) alkaloid hodgkinsine and preliminary assessment of their antinociceptive activityJ. Org. Chem.72(21)7909-7914(2007)
T69413	Primordazine B
	Primordazine B is a selective inhibitor of primordial germ cell (PGC) development which targets poly(A)-tail-independent noncanonical translation (PAINT).
T38209	Hodgkinsine
	Hodgkinsine is a pyrrolidinoindoline alkaloid that has been found inP. colorataand has analgesic activity.1It increases latency to paw licking in the hot plate test and latency to tail withdrawal in the tail-flick test in mice when administered at a dose of 5 mg/kg. 1.Amador, T.A., Verotta, L., Nunes, D.S., et al.Antinociceptive profile of hodgkinsinePlanta Med.66(8)770-772(2000)
T73742	98N12-5
	98N12-5 是一种新型的可电离脂质，用于siRNA 在体内高效传递到肝脏。
T35419	τ-Fluvalinate
	τ-Fluvalinate is a pyrethroid acaricide.1It induces tail currents in Western honeybee (A. mellifera) voltage-gated sodium channels (AmNav1) expressed inXenopusoocytes (EC50= 60 nM). It also induces tail currents in honeybee parasitic Varroa mite (V. destructor) Nav1 channels (VdNav1) expressed inXenopusoocytes (EC50= 160 nM) with a faster tail current decay than that of AmNav1 channels. Topical application of τ-fluvalinate (2 μl) in combination with coumaphos , atrazine , 2,4-DMPF, chlorpyrifos ...
T69857	DB293
	DB293 is an inhibitor of PIT-1 and BRN-3 transcription factors. DB293 binds as head-to-tail stacked dimers in the minor groove of 5'-ATGA sequence, thereby leading to an increase in the size of minor groove.
T39286	Br-PBTC
	Br-PBTC is a highly potent, 2/4 subtype-selective positive allosteric modulator of nicotinic acetylcholine receptors (nAChRs). It specifically targets α2β2, α2β4, α4β2, α4β4, (α4β2)2α4, and (α4β2)2β2 subtypes of nAChRs, with EC50 values ranging from 0.1 to 0.6 μM. Br-PBTC exerts its activity by binding to the c-tail region of an α subunit.
T71586	Z-VAE(OMe)-fmk
	Z-VAE(OMe)-fmk is a cell-permeable and irreversible UCHL1 inhibitor. The inhibitor approaches the active-site cleft from the opposite side of the crossover loop as compared to the direction of approach of ubiquitin's C-terminal tail, thereby occupying the P1' (leaving group) site, a binding site perhaps used by the unknown C-terminal extension of ubiquitin in the actual in vivo substrate(s) of UCHL1.
T75954	Mambalgin 1 TFA
	Mambalgin 1 TFA, a selective inhibitor of ASIC1a (with IC50 values of 192 nM for human ASIC1a and 72 nM for the ASIC1a/1b dimer), preferentially binds to the channel in its closed/inactive state. It demonstrates selectivity for ASIC1a over a range of other channels, including ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2, and Kv1.2. In vivo, Mambalgin 1 TFA effectively prolongs the latency of the withdrawal response in mouse tail-flick and paw-flick tests.
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
T61721	RAGE 229
	RAGE 229, N-(4-(7-cyano-4-(morpholin-4ylmethyl) quinolin-2-yl)phenyl)acetamide 是一种小分子 ctRAGE-DIAPH1抑制剂，具有口服活性。RAGE 229 可通过抑制 ctRAGE 与 DIAPH1 的相互作用来抑制细胞内 RAGE 信号。
T38055	Salvinorin A Propionate
	Salvinorin A propionate is a selective partial agonist at κ1-opioid receptors (KOR) with a Ki value of 32.6 nM. It inhibits adenylate cyclase (EC50 = 4.7 nM) in HEK293 cells transfected with human KOR. It is selective for KORs over μ, δ, and ORL-1 opioid receptors and has no effect at serotonin, dopamine, muscarinic, or adrenergic receptors. In mice, salvinorin A propionate (13 μg, i.c.v.) reduces nociceptive responses in a radiant heat tail-flick assay, though not as potently as salvinorin A .
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
T36719	D-NAME (hydrochloride)
	N(G)-Nitro-D-arginine methyl ester (D-NAME) is the less active enantiomer of the nitric oxide (NO) synthase inhibitor N(G)-nitro-L-arginine methyl ester . D-NAME was initially thought to be inactive and was often used as a negative control for L-NAME. Later studies showed that D-NAME (40 mg/kg/day in rats) can have similar but less pronounced effects as L-NAME (40 mg/kg/day in rats) in the cardiovascular system, particularly at long-term timepoints. D-NAME (3-10 &#181g/mouse) had no effect on no...
T79926	Poly(A) polymerase	DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	Poly(A) polymerase 通过使用 ATP 作为单元，催化在 RNA 的 3'末端顺序掺入 AMP，形成多聚腺苷尾，从而增强 RNA 稳定性并提升真核细胞 mRNA 的翻译效能。该酶具备高效的聚腺苷酸化活性，能在 RNA 3'端添加 20-200 个腺苷酸(A)单元。
TP2003	Mambalgin 1
	Selective ASIC1a inhibitor (IC50 values are 192 and 72 nM for human ASIC1a and ASIC1a/1b dimer, respectively). Binds to closed/inactive channel. Selective for ASIC1a over ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2 and Kv1.2 channels. Increases late
T83707	F9170 TFA
	F9170是一种抗病毒肽，对应HIV-1包膜糖蛋白的789-803氨基酸。它与HIV-1包膜蛋白胞浆尾部的LLP1域结合，并抑制HIV-1 IIIB对MT-2细胞的感染(EC50 = 0.19 µM)。在恒河猴模型的类人猿免疫缺陷病毒(SHIV)感染中，F9170 (3 mg/kg)能降低血浆病毒负荷。
T83685	UFP101 TFA
	UFP101是一种合成肽类物质，作为nociceptin受体的拮抗剂（Ki为0.06 nM，测试于表达人类受体的CHO细胞中）。它对nociceptin受体的选择性高于κ-opioid受体（Ki为204 nM，测试于表达大鼠受体的CHO细胞中）。UFP101能抑制表达于CHO细胞膜的nociceptin受体释放GTPγS（EC50为1.86 nM）。通过脑室内给药，UFP101（10 nmol/每只动物）能延长小鼠尾巴甩动试验中的尾巴撤回潜伏期。在由盲肠结扎和穿刺诱发的小鼠败血症模型中，UFP101（0.003、0.03及0.3 mg/kg）能提高生存率。
T83688	R 715 TFA [Ac-Lys-[D-βNal7,Ile8]des-Arg9]-BK,Ac-Lys-Arg-Pro-Pro-Gly-Phe-Ser-D2Nal-Ile-OH
	R 715是一种布拉迪肾上腺素B1受体拮抗剂。它抑制在表达布拉迪肾上腺素B1受体的孤立人类脐带中由布拉迪肾上腺素引发的收缩（pA2 = 8.49）。R 715（200、400及600 µg/kg）通过尾部闪烁测试减少了由链脲佐菌素（STZ）诱导的糖尿病神经病变小鼠模型中尾部撤回的潜伏期。它还在以髓磷脂少突胶质细胞糖蛋白（MOG）（35-55）（MOG35-55）抗原肽诱导的实验性自体免疫性脑炎（EAE）小鼠模型中，通过每天1 mg/kg的剂量减少了后肢无力和瘫痪的发病率，改善对称步态，并减少脊髓炎症灶点数、神经元脱髓鞘以及病灶单核细胞侵袭。R 715（0.01 nmol/动物，脑室内）能在自发性高血压大鼠中降低平均动脉血压并增加心率。
T38193	β-Endorphin (1-27) (human) (trifluoroacetate salt)
	β-Endorphin (1-27) is an endogenous peptide that binds to μ-, δ-, and κ-opioid receptors (Kis = 5.31, 6.17, and 39.82 nM, respectively, in COS-1 cells expressing rat receptors). It binds to rat and mouse brain membrane preparations (IC50s = 1.1 and 5.7 nM, respectively) and induces chemotaxis of human monocytes in vitro when used at a concentration of 1 nM. Intracerebroventricular administration of β-endorphin (1-27) increases the latency to tail withdrawal in response to thermal stimulation in ...
T36722	Deltorphin II (trifluoroacetate salt)
	Deltorphin II is a peptide agonist of δ2-opioid receptors.1,2It is selective for δ-opioid receptors over μ- and κ-opioid receptors in radioligand bindings assays (Kis = 0.0033, >1, and >1 μM, respectively) and induces [35S]GTPγS binding in mouse brain membrane preparations (EC50= 0.034 μM). Deltorphin II (0.12 mg/kg) decreases the infarction zone:risk zone ratio in a rat model of myocardial ischemia-reperfusion injury induced by coronary occlusion, an effect that can be reversed by the δ2-opioid...
T12738	Rivanicline hemioxalate RJR-2403 hemioxalate,(E)-Metanicotine hemioxalate	Others	Others
	Rivanicline hemioxalate (RJR-2403 hemioxalate; (E)-Metanicotine hemioxalate) 是一种神经元烟碱受体 (neuronal nicotinic receptor) 激动剂，对 α4β2 亚型有高度选择性(Ki= 26 nM)，比对于 α7 受体的选择性高1000倍(Ki=3.6 μM)。

化合物

Activated EG3 Tail

Cat.No: T83174

C13-113-tri-tail

Cat.No: T77267

C13-112-tetra-tail

Cat.No: T77268

C13-112-tri-tail

Cat.No: T77266

C13-113-tetra-tail

Cat.No: T77269

Amiodarone hydrochloride

Cat.No: T1496

Synonym: 盐酸胺碘酮,Amiodar,Amiodarone HCl,Nexterone

Target: Potassium Channel, Adrenergic Receptor, Autophagy

Mecamylamine hydrochloride

Cat.No: T2141

Synonym: 盐酸美加明,Inversine,Mevasin

Target: AChR

Cat.No: T1909

Synonym: 7-氯-4-羟基-3-(3-苯氧基)苯基-2(1H)-喹啉,L701324

Target: NMDAR, iGluR

Antimicrobial Compound 1

Cat.No: T10337

Target: Antibacterial

Cat.No: T3157

Synonym: RNR Inhibitor COH29

Target: DNA/RNA Synthesis

Dihydropteroyl hexaglutamate

Cat.No: T31475

Cat.No: T38210

Cat.No: T69413

Cat.No: T38209

Cat.No: T73742

Cat.No: T35419

Cat.No: T69857

Cat.No: T39286

Cat.No: T71586

Mambalgin 1 TFA

Cat.No: T75954

SRA880 free base

Cat.No: T28851

Synonym: SRA 880,NVPSRA880,NVP SRA880,NVP-SRA880,SRA-880,SRA880

Cat.No: T61721

Salvinorin A Propionate

Cat.No: T38055

SRA880 malonate

Cat.No: T26225

Synonym: SRA880,NVPSRA880,NVP-SRA880,NVP-SRA-880,NVP-SRA 880,NVP SRA880

D-NAME (hydrochloride)

Cat.No: T36719

Poly(A) polymerase

Cat.No: T79926

Target: DNA/RNA Synthesis

Cat.No: TP2003

Cat.No: T83707

Cat.No: T83685

Cat.No: T83688

Synonym: [Ac-Lys-[D-βNal7,Ile8]des-Arg9]-BK,Ac-Lys-Arg-Pro-Pro-Gly-Phe-Ser-D2Nal-Ile-OH

β-Endorphin (1-27) (human) (trifluoroacetate salt)

Cat.No: T38193

Deltorphin II (trifluoroacetate salt)

Cat.No: T36722

Rivanicline hemioxalate

Cat.No: T12738

Synonym: RJR-2403 hemioxalate,(E)-Metanicotine hemioxalate

Target: Others

Cat. No.	Product Name	Target	Signaling Pathways
T83913	Mitraciliatine
	Mitraciliatine是一种在M. speciosa（泰国称为Kratom）中发现的生物碱，是μ-阿片受体（MOR）部分激动剂和κ-阿片受体（KOR）激动剂。该化合物对MOR和KOR具有选择性，与δ-阿片受体（DOR; EC50s分别为228, 218, 和 >1,000 nM，针对小鼠受体在GTPγS结合实验中的表现）。Mitraciliatine（100 nmol/动物，脑室内注射）在小鼠的热水尾部缩回实验中延长了撤回潜伏期，这一效果可以通过敲除MOR而非KOR来逆转。与吗啡不同，Mitraciliatine不会诱发过度活动或呼吸抑制。

天然产物

Cat.No: T83913

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