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13

抑制剂 & 化合物

10

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T3198L	PRE-084 hydrochloride	Sigma receptor	GPCR/G Protein
	PRE-084 hydrochloride 是 σ1 的选择性激动剂在sigma 受体检测中，IC50值为44 nM。
T23394	SR 57227A SR57227盐酸盐,SR 57227 hydrochloride	5-HT Receptor	GPCR/G Protein; Neuroscience
	SR 57227A (SR 57227 hydrochloride) 是一种有效的、具有口服活性和选择性的 5-HT3 受体激动剂，具有穿越血脑屏障的能力和抗抑郁作用。它对大鼠皮质膜和整个 NG 108-15 细胞或其膜上的 5-HT3 受体结合位点的亲和力，IC50在 2.8 至 250 nM 之间。
T3486	3-MATIDA	GluR; NMDAR	Neuroscience
	3-MATIDA 是一种有效的 mGluR-1 拮抗剂（IC50：6.3 μM，大鼠 mGluR-1a）。显示出 ≥ 40 倍于其他受体的选择性：mGluR-5、mGluR-2、mGluR-4 (mGluR-4a) (IC50 > 300 μM)、NMDA 和 GluR (AMPA) (IC50 = 250 μM)。 3-MATIDA 在体外培养的鼠皮质细胞和大鼠海马切片培养物中充当神经保护剂。
T3648	Hypidone hydrochloride YL0919	5-HT Receptor	GPCR/G Protein; Neuroscience
	Hypidone hydrochloride (YL0919) 是一种新型抗抑郁候选药物，具有作为 5-HT1A 受体激动剂和选择性 5-羟色胺再摄取抑制剂的双重活性。
T16155	MSN-125	Akt	Cytoskeletal Signaling; PI3K/Akt/mTOR signaling
	MSN-125 effectively inhibits Bax/Bak-mediated apoptosis in HCT-116, BMK Cells, and primary cortical neurons protect primary neurons against glutamate excitotoxicity. MSN-125 is an effective Bax and Bak oligomerization inhibitor. MSN-125 prevents mitochond
T28850	SR57227A SR 57227A,SR-57227A
	SR 57227A is a highly selective of peripheral and central 5-HT3 receptors and an inhibitor of NMDA receptor-mediated responses in rat cortical pyramidal cells. It exhibits anti-depressant like effects in rats and decreased isolation-induced aggressive beh
T37661	LY 2886721 Hydrochloride
	Potent and selective β-secretase (BACE) inhibitor (IC50 values are 10.2 and 20.3 nM for human BACE2 and BACE1, respectively). Displays >5,000-fold selectivity for BACE over other proteases including cathepsin D, pepsin and renin. Inhibits Aβ1-40 and Aβ1-42 production in cells expressing mutated APP. Reduces hippocampal and cortical Aβ and sAPPβ levels in an Alzheimer's disease mouse model.
T36516	RC574 RC574
	RC574 is an inhibitor of ferroptosis and a derivative of the antioxidant and hypocholesterolemic agent probucol .1It inhibits glutamate-induced cell death in HT22 cells (IC50= 276.2 nM) and mouse primary cortical neurons when used at a concentration of 3 μM. RC574 (3 μM) increases glutathione peroxidase 1 (GPX1) levels and GPX activity, as well as inhibits glutamate-induced mitochondrial superoxide anion production, in HT22 cells. It completely inhibits ferroptosis induced by the GPX4 inhibitor ...
T37370	Amyloid-β (25-35) Peptide (human) (trifluoroacetate salt)
	Amyloid-β (25-35) (Aβ (25-35)) is an 11-residue fragment of the Aβ protein that retains the physical and biological characteristics of the full length peptide. It forms fibrils that react to thioflavin T and Congo red and are organized in a cross-β arrangement of β-strands similar to Aβ (1-40) and Aβ (1-42) fibrils. Aggregated Aβ (25-35) decreases the viability of rat adrenal PC12 cells. It also decreases the viability of primary rat cortical neurons at concentrations ranging from 1 nM to 30 μM....
T35494	(±)11(12)-EET
	(±)11(12)-EET is a fully racemic version of the R/S enantiomeric forms biosynthesized from arachidonic acid by cytochrome P450 enzymes.[1][2][3[]A higher proportion of 11(R),12(S)-EET is produced by the CYP450 isoforms CYP2C23 and CYP2C24 while CYP2B2 produces a higher proportion of 11(S),12(R)-EET.[3]11(12)-EET has been shown, along with 8(9)-EET to play a role in the recovery of depleted calcium pools in cultured smooth muscle cells[4] It also inhibits basolateral 18-pS potassium channels in t...
T37215	5α,6β-Dihydroxycholestanol
	5α,6β-Dihydroxycholestanol is an oxysterol metabolite of cholesterol formed from conversion of cholesterol epoxides by 5,6-epoxysterol hydrolase. It inhibits NMDA-mediated calcium influx in HEK293 cells expressing NR1/NR2B NMDA receptors in a concentration-dependent manner. It also binds to voltage-gated sodium (Nav) channels and decreases action potentials in hippocampal neurons in vitro when used at a concentration of 10 uM. It increases survival of spinal cord motoneurons, cortical neurons, a...
T36570	KUS121
	KUS121 is a valosin-containing protein (VCP) modulator that inhibits VCP ATPase activity (IC50= 330 nM).1It inhibits cell death, ATP depletion, and upregulation of C/EBP-homologous protein (CHOP) induced by tunicamycin, an inducer of ER stress, in HeLa cells when used at concentrations of 20, 50, and 50 μM, respectively. KUS121 (100 μM) inhibits ATP depletion and cell death induced by oxygen-glucose deprivation (OGD) in rat primary cortical neurons in anin vitromodel of cerebral ischemia.2It red...
T36903	Rasagiline-13C3 (mesylate) Rasagiline-13C3 (mesylate)
	Rasagiline-13C3is intended for use as an internal standard for the quantification of rasagiline by GC- or LC-MS. Rasagiline is an inhibitor of monoamine oxidase B (MAO-B; IC50= 4.43 nM for the rat brain enzyme).1It is selective for MAO-B over MAO-A (IC50= 412 nM for the rat brain enzyme). It inhibits serum and NGF withdrawal-induced apoptosis of PC12 cells when used at concentrations ranging from 0.01 to 100 μM.2Rasagiline inhibits rat brain MAO-Bin vivo(ED50= 0.1 mg/kg).1It reduces cerebral ede...

化合物

PRE-084 hydrochloride

Cat.No: T3198L

Target: Sigma receptor

Cat.No: T23394

Synonym: SR57227盐酸盐,SR 57227 hydrochloride

Target: 5-HT Receptor

Cat.No: T3486

Target: GluR, NMDAR

Hypidone hydrochloride

Cat.No: T3648

Synonym: YL0919

Target: 5-HT Receptor

Cat.No: T16155

Target: Akt

Cat.No: T28850

Synonym: SR 57227A,SR-57227A

LY 2886721 Hydrochloride

Cat.No: T37661

Cat.No: T36516

Synonym: RC574

Amyloid-β (25-35) Peptide (human) (trifluoroacetate salt)

Cat.No: T37370

Cat.No: T35494

5α,6β-Dihydroxycholestanol

Cat.No: T37215

Cat.No: T36570

Rasagiline-13C3 (mesylate)

Cat.No: T36903

Synonym: Rasagiline-13C3 (mesylate)

Cat. No.	Product Name	Target	Signaling Pathways
T6S1418	Praeruptorin C	Antioxidant; Calcium Channel	Membrane transporter/Ion channel; Metabolism; oxidation-reduction
	Praeruptorin C 是白花前胡中的一种主要成分，是钙拮抗剂，pD2′值为 5.7。
T5S2129	Sciadopitysin	TNF; NF-κB	Apoptosis; NF-κB
	Sciadopitysin 是一种双黄酮类化合物，来自银杏叶片中。它通过抑制NF-κB 活化并降低c-Fos 和NFATc1的表达来抑制 RANKL 诱导的破骨细胞生成和骨丢失。
TN2037	Paeonilactone C (3S,3AR,6S,7AR)-3-[(苯甲酰基氧基)甲基]四氢-6-羟基-6-甲基-2,5(3H,4H)-苯并呋喃二酮,芍药内苷 C	Others	Others
	Paeonilactone C significantly protects primary cultures of rat cortical cells against H2O2-induced neurotoxicity.
TN5169	Traxillaside 香榧	Others	Others
	Traxillaside has significant neuroprotective activities against glutamate-induced toxicity in primary cultures of rat cortical cells .
TN3771	Dasycarpol	Others	Others
	Dasycarpol(9beta-Hydroxyfraxinellone) shows significant neuroprotective activity against glutamate-induced neurotoxicity in primary cultures of rat cortical cells at a concentration of 0.1 microM. Dasycarpol also shows moderate inhibitory activity on lung
TCA2511	11Beta-hydroxyprogesterone	Sodium Channel	Membrane transporter/Ion channel
	The progesterone derivatives 11 alpha- and 11 beta-hydroxyprogesterone are potent inhibitors of 11 beta-hydroxysteroid dehydrogenase (isoforms 1 and 2) in vitro and can confer mineralocorticoid activity on corticosterone in the rat in vivo. 11beta-Hydroxyprogesterone acts as a mineralocorticoid agonist in stimulating Na+ absorption in mammalian principal cortical collecting duct cells.
TN2036	Paeonilactone B (+)-Paeonilactone B	NADPH-oxidase	Immunology/Inflammation
	Paeonilactone B ((+)-Paeonilactone B) 是一种来自白芍的单萜类化合物，具有神经保护活性，抑制氧化应激，在大鼠皮质细胞在抑制 H2O2 诱导的神经毒性。
T16846	Sauristolactam Saurolactam	Others	Others
	Sauristolactam inhibits the receptor activator of nuclear factor-κB ligand (RANKL)-induced osteoclastogenesis and has the potential to inhibit osteoclast differentiation. Sauristolactam, a natural aristolactam isolated from aerial portions of Saururus Chi
TN3444	Aristolactam BII	HIV Protease	Microbiology/Virology; Proteases/Proteasome
	Aristolactam BII exhibits antimicrobial and antiinflammatory activity, it shows significant activity towards DPPH radical scavenging and potent inhibitory effects against tyrosinase mushroom. Aristolactam BII also exerts its significant neuroprotective ef
TN5164	trans-Hinokiresinol	IL Receptor; TNF; NOS; LTR	Apoptosis; Immunology/Inflammation
	Hinokiresinol is a novel inhibitor of LTB4 binding to the human neutrophils, it has antiallergic effect, it inhibits IgE-induced mouse passive cutaneous anaphylaxis reaction. Hinokiresinol (trans-hinokiresinol) and nyasol (cis-hinokiresinol) are estrogen

天然产物

Cat.No: T6S1418

Target: Antioxidant, Calcium Channel

Cat.No: T5S2129

Target: TNF, NF-κB

Paeonilactone C

Cat.No: TN2037

Synonym: (3S,3AR,6S,7AR)-3-[(苯甲酰基氧基)甲基]四氢-6-羟基-6-甲基-2,5(3H,4H)-苯并呋喃二酮,芍药内苷 C

Target: Others

Cat.No: TN5169

Synonym: 香榧

Target: Others

Cat.No: TN3771

Target: Others

11Beta-hydroxyprogesterone

Cat.No: TCA2511

Target: Sodium Channel

Paeonilactone B

Cat.No: TN2036

Synonym: (+)-Paeonilactone B

Target: NADPH-oxidase

Cat.No: T16846

Synonym: Saurolactam

Target: Others

Aristolactam BII

Cat.No: TN3444

Target: HIV Protease

trans-Hinokiresinol

Cat.No: TN5164

Target: IL Receptor, TNF, NOS, LTR

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