Neurological Disease

SIB-1757 is a highly selective and noncompetitive antagonist of mGlu5 receptor with an IC₅₀ of 0.4 μM.

TROX-1 is a selective, orally active and brain-penetrant N-type calcium channel (Cav2.2) inhibitor with an IC₅₀ value of 0.11 μM. TROX-1 exerts state-dependent and use-dependent inhibition, preferentially targets open/inactivated channels, blocks depolarization-associated calcium influx, and fully blocks calcium influx in rat dorsal root ganglion neurons. TROX-1 reverses inflammatory-induced hyperalgesia, nerve injury-induced allodynia. TROX-1 can be used for the research of pain.

Sofpironium bromide (BBI 4000) is an anticholinergic agent used in the study of primary axillary hyperhidrosis (PAH). Sofpironium bromide reduces sweating by inhibiting M3 muscarinic receptors in eccrine glands at the application site. Sofpironium bromide also has a high afnity for the M1, M2, M4 and M5 subtypes.

D-NMAPPD ((1R,2R)-B13) is an acid ceramidase inhibitor. D-NMAPPD regulates NMDA receptor properties by enhancing endogenous production of ceramides. D-NMAPPD has anticancer effecs.

Homatropine Bromide is an orally active muscarinic acetylcholine receptor antagonist and can be used as an anticholinergic agent.

TrkA-IN-3 is a potent, subselective and allosteric TrkA inhibitor, with an IC₅₀ of 22.4 nM. TrkA-IN-3 shows more than 8000-fold selectivity for TrkA over TrkB and TrkC. TrkA-IN-3 can be used for the research of pain.

GR 103691 is a potent, selective dopamine D₃ receptor antagonist with a K_i value of 0.4 nM. GR 103691 shows more than 100-fold selectivity for human dopamine human (h)D₃ over hD₄ and hD₁ sites.

DALDA acetate is a potent and highly selective μ-opioid receptor agonist with a K_i of 1.69 nM. DALDA acetate shows antinociceptive and respiratory effects.

Sarizotan (EMD 128130) is an orally active serotonin 5-HT_1A receptor and dopamine receptor agonist. Sarizotan (EMD 128130) exhibits IC₅₀ values of 6.5 nM (rat 5-HT_1A), 0.1 nM (human 5-HT_1A), 15.1 nM (rat D₂), 17 nM (human D₂), 6.8 nM (human D₃) and 2.4 nM (human D_4.2), respectively.

NCC-149 is a selective HDAC8 inhibitor and can be used for neural differentiation research.

CART(55-102)(human) is an endogenous satiety factor with potent appetite-suppressing activity. CART(55-102)(human) is closely associated with leptin and neuropeptide Y.

Darglitazone (CP-86325), a thiazolidinedione, is a potent, selective, and orally active PPAR-γ agonist. Darglitazone is effective in controlling blood glucose and lipid metabolism, and can be used for type II diabetes research.

Almitrine mesylate, a peripheral chemoreceptor agonist, inhibits selectively the Ca²⁺-dependent K⁺ channel.

Ropivacaine-d₇ is deuterium labeled Ropivacaine. Ropivacain is a potent?sodium channel?blocker. Ropivacain blocks impulse conduction via reversible inhibition of?sodium ion influx?in nerve fibrese. Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC₅₀ of 402.7 μM in COS-7 cell's membrane. Ropivacaine is used for the research of neuropathic pain?management.

Dimemorfan phosphate is a sigma 1 receptor agonist, used as a potent antitussive.

Asiaticoside (Standard) is the analytical standard of Asiaticoside. This product is intended for research and analytical applications. Asiaticoside, a trisaccaride triterpene from Centella asiatica, suppresses TGF-β/Smad signaling through inducing Smad7 and inhibiting TGF-βRI and TGF-βRII in keloid fibroblasts; Asiaticoside shows antioxidant, anti-inflammatory, and anti-ulcer properties.

ABT-702 (Adenosine Kinase Inhibitor) is a potent, orally active, and selective adenosine kinase (AK) inhibitor with an IC₅₀ of 1.7 nM. ABT-702 shows >1300-fold selectivity for AK over other biological targets, including cyclooxygenases-1 and -2. ABT-702 attenuates inflammation in diabetic retinopathy by increasing free adenosine levels. ABT-702 shows analgesic and anti-inflammatory effects in vivo. ABT-702 can be used for diabetic retinopathy research.

Nε-(Carboxyethyl) lysine is an advanced glycation end product (AGE). Nε-(Carboxyethyl) lysine induces cross-linking between proteins, thereby affecting protein structure and function and causing protein denaturation. Nε-(Carboxyethyl) lysine binds to the RAGE receptor, affects cell signal transduction, and regulates processes such as inflammatory responses, cell proliferation, and apoptosis. Nε-(Carboxyethyl) lysine affects glutamate transporters, reduces glutamate uptake and S100β protein secretion, influences neurotransmission in the nervous system, and exhibits diabetes-related neurotoxicity.

Fimasartan (BRA-657) is an orally effective angiotensin receptor AT1 non-peptide antagonist. Fimasartan has antihypertensive effects. Fimasartan improves neuroinflammation and brain injury mediated by NLRP3 inflammatome after intracerebral hemorrhage, and has neuroprotective effect. Fimasartan inhibits the expression of inducible nitric oxide synthase through the inactivation of NF-κB and activator protein-1.

Intepirdine (SB742457) is a highly selective 5-HT6 receptor antagonist with pKi of 9.63; exhibits >100-fold selectivity over other receptors.