About 30 results found for searched term "SANT-1" (0.102 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M2997 | SANT-1 | Smo |
| SANT-1 directly binds to Smoothened (Smo) receptor with Kd of 1.2 nM and inhibits Smo agonist effects with IC50 of 20 nM. | ||
| M1831 | Cyclosporine A | Immunology/Inflammation |
| Cyclosporine | ||
| Cyclosporin A is an immunosuppressant that binds to cyclophilin and inhibits calcineurin with an IC50 of 7 nM. cyclosporin A [CsA] binds to the cyclophilin 18 (Cyp18)-CsA complex. the Cyp18-CsA complex recruits calcium-regulated neurophosphatase (CaN), leading to the blocking of cytokine gene transcription in activated T cells. CsA is a highly specific inhibitor of T-cell activation. | ||
| M4247 | Schizandrol-B | PCSK9 |
| Gomisin-B; Schizantherin-B; Wuweizi ester-B; Schisantherin-B | ||
| Schisantherin B (Gomisin-B; Wuweizi ester-B; Schisantherin-B) is a lignan from Schisandra chinensis that promotes liver enlargement in mice through activation of the PXR and YAP pathways and inhibits PCSK9 protein expression with an IC50 value of 1.10 μM. | ||
| M4500 | Crocin-II | NO Synthase |
| Crocin II, isolated from the fruit of Gardenia jasminoides, has antioxidant, anticancer and antidepressant activities. Crocin II inhibited NO production with IC50 value of 31.1 μM. Crocin II inhibited the expression of iNOS and COX-2 protein and M-RNA. | ||
| M4876 | Vidofludimus | DHODH |
| SC12267, 4SC-101 | ||
| Vidofludimus(4SC-101; SC12267) is an immunosuppressant that inhibits DHODH and inhibits il-17 secretion without affecting lymphocyte proliferation. | ||
| M7640 | Bisantrene | Others |
| CL216942 | ||
| Bisantrene is an antineoplastic agent, MDR1 substrate, DNA intercalator, and topoisomerase II poison. | ||
| M7836 | Hyperforin | TRP Channel |
| Hyperforin is a transient receptor typical 6 (TRPC6) channel activator that regulates Ca2+ levels by activating Ca2+-transducing non-selective typical TRPC6 channels, with antidepressant and antitumor activities. In addition, Hyperforin modulates IL-17α secretion from γδ T cells and ameliorates Imiquimod-induced skin inflammation in psoriasis-like mice. | ||
| M9263 | CY-09 | Pyroptosis |
| CY09 | ||
| CY-09 is a selective direct inhibitor of NLRP3 with anti-inflammatory and antidepressant activity, which inhibits inflammatory cytokine production and TRPA1 activation by inhibiting the activation of the NLRP3 inflammatory vesicle, thereby decreasing the intracellular Ca2+ level and reducing the pro-inflammatory polarization of macrophages, alleviating pain and injury in animals. In addition, CY-09 can inhibit pyroptosis. | ||
| M10608 | NLX-101 (F-15599) | 5-HT Receptor |
| NLX101 | ||
| NLX-101 (F-15599) is a highly selective G-protein biased 5-HT1A receptor agonist, with Ki of 3.4 nM. NLX-101 (F-15599) mediates antidepressant-like activity in rats via prefrontal cortex 5-HT 1A receptors. NLX-101 (F-15599) has over 1000-fold higher affinity for this target over other receptors. | ||
| M10714 | Pitolisant | Histamine Receptor |
| Tiprolisant | ||
| Pitolisant is a potent and selective non-imidazole recombinant hentistamine H3 receptor reversed agonist,Ki 0.16 nM. | ||
| M10855 | Mephenytoin | Others |
| Mephenytoin is an anticonvulsant that is a substrate for CYP2C19 and CYP2B6. | ||
| M11253 | BD750 | JAK |
| BD750 is an effective immunosuppressant of JAK3/STAT5 and inhibits IL-2-induced JAK3/ STAT5-dependent T cell proliferation with IC50 values of 1.5 μM and 1.1 μM in mice and human T cells, respectively. | ||
| M13408 | SNAP 94847 hydrochloride | Others |
| SNAP 94847 Hydrochloride is a novel high affinity selective melanin concentration hormone receptor 1 (MCHR1) antagonist with antidepressant like activity. SNAP 94847 Hydrochloride is a high-affinity antagonist (pA2=7.81) of MYo-inositol phosphate formation induced by MCH. | ||
| M13996 | Pitolisant hydrochloride | Histamine Receptor |
| Ciproxidine; BF 2649 | ||
| Pitolisant hydrochloride is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM). | ||
| M18932 | α-Spinasterol | TRP Channel |
| α-Spinasterol is a transient receptor potential vanilloid 1 (TRPV1) antagonist, has anti-inflammatory, antidepressant, antioxidant and antinociceptive effects. α-Spinasterol inhibits COX-1 andCOX-2 activities with IC50 values of 16.17 μM and 7.76 μM, respectively. | ||
| M20795 | Oxolamine Citrate | Cytochrome P450 (e.g. CYP17) |
| SKF-9976 citrate, AF-438 citrate | ||
| Oxolamine (SKF-9976, AF-438) citrate, a cough suppressant, is an inhibitor of CYP2B1/2. Oxolamine citrate also exhibits anti-inflammatory effect. | ||
| M21160 | ARD-61 | PROTAC |
| ARD-61 is a potent and specific PROTAC androgen receptor (AR) depressant. ARD-61 effectively and efficiently induces AR and progesterone receptor (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and also effectively inhibits tumor growth in a mouse MDA-MB-453 xenograft model. | ||
| M21435 | MS170 | PROTAC |
| MS170 is a potent selective PROTAC AKT depressant. MS170 consumes total AKT (T-AKT) and has a DC50 value of 32 nM. MS170 binds to AKT1, AKT2 and AKT3 with Kd of 1.3 nM, 77 nM and 6.5 nM, respectively. | ||
| M21512 | SR-1114 | PROTAC |
| SR-1114 is a first-in-class PROTAC ENL depressant. SR-1114 in MV4; ENL degradation was observed in 11, MOLM-13 and OCI/AML-2 cells with DC50 values of 150 nM, 311 nM and 1.65 μM, respectively. | ||
| M21519 | U7D-1 | PROTAC |
| U7D-1 is a first-in-class, potent and selective ubiquitin-specific protease 7 USP7 PROTAC depressant in RS4; The DC50 in 11 cells was 33 nM. U7D-1 has anti-cancer activity. | ||
| M22501 | SM-102 | Liposome |
| SM102 | ||
| ALC-0159 is a lipid conjugate of polyethylene glycol that can be used as an immunosuppressant SM-102 is an ionizable aminolipid with a terminal hydroxyl group in the head group, which reduces the hydration of the head group and improves hydrogen bonding interactions with nucleic acids, thus enhancing transfection.SM-102 can be used for the preparation of lipid nanoparticles (LNPs), as well as for the lipid nanoparticle delivery of | ||
| M27613 | Irdabisant hydrochloride | Histamine Receptor |
| CEP-26401 hydrochloride | ||
| Irdabisant (CEP-26401) hydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant hydrochloride has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. | ||
| M27614 | Irdabisant | Histamine Receptor |
| CEP-26401 | ||
| Irdabisant (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used to research schizophrenia or cognitive impairment. | ||
| M27660 | Maprotiline | Autophagy |
| Maprotiline is a highly selective noradrenergic reuptake blocker, has strong antidepressant efficacy. Maprotiline induces cancer cells apoptosis by targeting ERK signaling pathway and CRABP1. Maprotiline restrains cell proliferation and metastasis, exhibits anticancer effect. | ||
| M28322 | Samelisant | Histamine Receptor |
| SUVN-G3031 | ||
| Samelisant (SUVN-G3031) is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant can be used for the research of sleep-related disorders. | ||
| M28323 | Samelisant free base | Histamine Receptor |
| SUVN-G3031 free base | ||
| Samelisant (SUVN-G3031) free base is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant free base has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant free base can be used for the research of sleep-related disorders. | ||
| M28813 | Ro 25-6981 | GluR |
| Ro 25-6981 is a potent, selective and activity-dependent NR2B subunit specific NMDA receptor antagonist. Ro 25-6981 shows anticonvulsant and anti-parkinsonian activity. Ro 25-6981 has the potential for the research of parkinson's disease (PD). | ||
| M29275 | Cipralisant | Histamine Receptor |
| GT-2331 | ||
| Cipralisant (GT-2331) is an orally active, low-toxicity, potent, selective, high affinity histamine H3 receptor full antagonist in vivo, and an agonist in vitro, with a pKi of 9.9 for histamine H3 receptor and a Ki of 0.47 nM for rat histamine H3 receptor. Cipralisant has the potential for attention-deficit hyperactivity disorder research. | ||
| M29397 | Cipralisant maleate | Histamine Receptor |
| GT-2331 maleate | ||
| Cipralisant (GT-2331) (maleate) is an orally active, low-toxicity, potent, selective, high affinity histamine H3 receptor full antagonist in vivo, and an agonist in vitro, with a pKi of 9.9 for histamine H3 receptor and a Ki of 0.47 nM for rat histamine H3 receptor. Cipralisant (maleate) has the potential for attention-deficit hyperactivity disorder research. | ||
| M30309 | Setiptiline | 5-HT Receptor |
| Org-8282 | ||
| Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine. | ||
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