Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T1111 |
Pralidoxime Chloride
2-PAM chloride,吡啶醛肟甲氯,2-Pyridinealdoxime methochloride,2-PAM (chloride) |
AChE | Neuroscience |
Pralidoxime Chloride (2-PAM chloride) 是一种肟类化合物,对中毒乙酰胆碱酯酶具有恢复作用,可用于有机磷中毒的研究。 | |||
T37428 |
TRPC6-PAM-C20
TRPC6-PAM-C20,3-(6,7-Dimethoxy-3,3-dimethyl-3,4-dihydro-isoquinolin-1-yl)-chromen-2-one |
TRP/TRPV Channel | Membrane transporter/Ion channel |
TRPC6-PAM-C20 是一种选择性 TRPC6 正变构调节剂。 TRPC6-PAM-C20 在表达 TRPC6 的 HEK 细胞中诱导胞内 Ca2+ 瞬时增加,EC50 为 2.37 μM。 TRPC6-PAM-C20 增强 OAG 诱导的血小板聚集。 | |||
T22404 |
Pralidoxime Iodide
2-PAM,碘解磷定 |
Others | Others |
Pralidoxime Iodide, also named 2-PAM, is an antidote approved for reactivation of inhibited acetylcholinesterase (AChE) in organophosphate poisoning. | |||
T70460 |
HM5023507
|
||
HM5023507, an orally active dual inhibitor of δγ isoforms in immune signaling. HM5023507 inhibited PI3Kδ and PI3Kγ isoforms with greater than 100-fold selectivity against PI3Kα and PI3Kβ in recombinant enzymatic assays and in primary human immune cells with an exquisite selectivity against other targets. | |||
T37075 |
CB2R PAM
Ec2la |
Cannabinoid Receptor | GPCR/G Protein |
CB2R PAM 是一种口服活性大麻素 2 型受体(CB2Rs)阳性突变调节剂,它能增强 CP 55940 和 2-Arachidonylglycerol 刺激的 [35S]GTPγS 与 CB2 受体的结合,但在没有激动剂的情况下没有作用。CB2R PAM 在神经病理性疼痛小鼠模型中显示出抗损伤活性。 | |||
T8741 |
MitoBloCK-10
3-fluoro-N'-[(E)-(5-nitrothiophen-2-yl)m |
Others | Others |
MitoBloCK-10 (3-fluoro-N'-[(E)-(5-nitrothiophen-2-yl)m) 是第一个能够减弱PAM 复合体活性的小分子调节剂,对 C 末端结构域的Tim44与前体和 Hsp70 结合具有抑制作用。 | |||
T23440 |
TC-N 22A
|
GluR | Neuroscience |
TC-N 22A 是一种作用力强的、可选择的、口服具有活性的、可以通过血脑屏障的 mGlu4 正向别构调节剂 (PAM)。TC-N 22A 在表达人 mGlu4 的 BHK 细胞中 EC50 表现为 9 nM。TC-N 22A 在激动和正向别构模型中对 mGlu 1、2、3、5 和 7 受体的活性表现很低 (EC50 >10 μM)。TC-N 22A 可以用于中枢神经系统疾病的研究。 | |||
T2067 |
NS11394
NS 11394 |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
NS11394 是可口服GABAA 的阳性变构调节剂 (PAM),Ki 值为 0.5 nM。它对GABAA 的选择性依次为 α5、α3、α2 和α1 受体,具有抗炎和抗焦虑活性。 | |||
T36520 |
COR659
|
Cannabinoid Receptor; GABA Receptor | GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience |
COR659 是一种有效的 GABAB 的阳性变构调节剂。COR659具有缓解大鼠对酒精和巧克力成瘾的作用。 | |||
T15618 | JNJ-46281222 | GluR | Neuroscience |
JNJ-46281222 is an metabotropic glutamate (mGlu) 2-selective, highly potent PAM (positive allosteric modulator). It has nanomolar affinity (Kd = 1.7 nM) and a high modulatory potency (pEC50 = 7.71). | |||
T80635 | Gentisuric acid | Drug Metabolite | Metabolism |
Gentisuric Acid,作为Aspirin的代谢产物同时也是α-酰胺化单加氧酶(PAM)的底物,可抵御Mitomycin C导致的DNA损伤。 | |||
T35081 |
VU0486321
VU 0486321,VU-0486321 |
||
VU0486321 is a potent mGlu1 PAM with moderate rat PK (CLp = 13.3. mL/min/kg,t1/2 = 54 min), good free fraction (human fu = 0.05, rat fu =0.03) and excellent CNS penetration (Kp = 1.02). | |||
T60763 | MMG-11 quarterhydrate | ||
MMG-11 quarterhydrate 是人TLR2的选择性拮抗剂,可抑制 TLR2/1 和 TLR2/6 信号,且细胞毒性低。MMG-11 quarterhydrate 对 Pam3CSK4诱导的 hTLR2/1 和 Pam2CSK4诱导的 hTLR2/6 反应的IC50值分别为 1.7 μM 和 5.7 μM。 | |||
T39771 |
nAChR agonist CMPI hydrochloride
|
||
nAChR agonist CMPI hydrochloride is a potent and selective positive allosteric modulator (PAM) of nAChR containing a α4:α4 subunit interface. nAChR agonist CMPI hydrochloride enhances the response of (α4) 3 (β2) 2 nAChR to ACh (10 μM) with an EC 50 of 0.26 μM. nAChR agonist CMPI hydrochloride has potential for the research of nicotine dependence and many neuropsychiatric conditions associated with decreased brain cholinergic activity. |