Ionizable Lipid Products

CLP290 is an orally available activator of the neuron-specific K+-Cl− cotransporter KCC2, displays potential for treatment of a wide range of neurological and psychiatric indications. CLP290 can significantly lower blood arginine-vasopressin (AVP) and glucose levels in STZ rats[1][2].

F17464 is a dopamine D3 receptor preferential antagonist exhibiting high affinity for human dopamine receptor subtype 3 (hD3) (Ki=0.17 nM) and 5-HT1a (Ki=0.16 nM) and a >50 fold lower affinity for the human dopamine receptor subtype 2 short and long form (hD2s/l) (Ki=8.9 and 12.1 nM, respectively). F17464 is a D3 receptor antagonist, 5-HT1a receptor partial agonist. F17464 blocks ketamine induced morphological changes, an effect D3 receptor mediated, in human dopaminergic neurons. F17464 increases dopamine release in the rat prefrontal cortex and mouse lateral forebrain-dorsal striatum and seems to reduce the effect of MK801 on % c-fos mRNA medium expressing neurons in cortical and subcortical regions. F17464 also rescues valproate induced impairment in a rat social interaction model of autism, with dose range 0.32-2.5 mg/kg i.p. in both rats and mice

Bay K 8644, a dihydropyridine compound, is a specific L-type Ca2+ channel agonist. Bay K 8644 increases Ca2+ influx through sarcolemmal Ca2+ channels by increasing the open time of the channel[1].

ATI-2341, pepducin targeting the C-X-C chemokine receptor type 4 (CXCR4), is an allosteric agonist activating the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization.

Evacetrapib is a potent and selective of CETP inhibitor, which inhibits human recombinant CETP protein (IC50 5.5 nM) and CETP activity in human plasma (IC50 36 nM) in vitro.

AZD1152-HQPA is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay, and appr 3700 fold more selective for Aurora B over Aurora A.

Bezuclastinib (PLX 9486; CGT9486) is a potent inhibitor of c-kit and c-kit D816V (0.0001<IC50<1 μM; extracted from patent WO2014100620 A2, compound P-2007). Bezuclastinib is a tyrosine kinase inhibitor.

Antioxidant 1024 (MD 1024) is an antioxidant agent and metal deactivator.

LUNA18 is an 11-mer cyclic peptide inhibitor for the intracellular tough target RAS with Kd (KRAS/G12D) of 0.043 nM and cellular IC50 of 1.4 nM (AsPC-1). LUNA18 orally and dose-dependently exhibits potent anti-cancer activities in a mouse xenograft model. LUNA18 shows 21–47% oral bioavailability in animals such as mouse, rat, monkey, and dog and notably does not require special formulations.

For the detailed information of Pregabalin, the solubility of Pregabalin in water, the solubility of Pregabalin in DMSO, the solubility of Pregabalin in PBS buffer, the animal experiment（test） (test) of Pregabalin, the cell expriment (test) of Pregabalin, the in vivo, in vitro and clinical trial test of Pregabalin, the EC50, IC50,and Affinity of Pregabalin,, please contact DC Chemicals.

NSC112200 is a chemical inhibitor of the EZH2 deubiquitinase ZRANB1 (at 10 uM), destabilizes EZH2, promotes proteasomal degradation of EZH2 and inhibits the viability of TNBC cells; NSC112200 is a mixture of 2,5-dibromo-3,6-dimethyl-1,4- benzenediol and 2,5-dibromo-3,6-dimethyl-1,4-benzoquinone.

Sirpiglenastat (DRP-104) is a broad acting glutamine antagonist. Sirpiglenastat has anticancer effects by directly targeting tumor metabolism and simultaneously inducing a potent antitumor immune response.

RX-3117(TV-1360; Fluorocyclopentenylcytosine) is novel a cytidine analog; shows anticancer activity in several cancer cell lines, including gemcitabine-resistant variants.

Axitinib is a multi-targeted tyrosine kinase inhibitor with IC50s of 0.1, 0.2, 0.1-0.3, 1.6 nM for VEGFR1, VEGFR2, VEGFR3 and PDGFRβ, respectively.

SBI-797812 is an orally active nicotinamide phosphoribosyltransferase (NAMPT) activator. SBI-797812 shifts NAMPT to NMN formation, increases NAMPT affinity for ATP, stabilizes phosphorylated NAMPT, promotes consumption of the pyrophosphate by-product, and blunts feedback inhibition by NAD+. SBI-797812 increases intracellular nicotinamide mononucleotide (NMN) and elevates liver NAD+ in mice.

TY-52156 is a potent S1P3 receptor antagonist in a competitive manner, and the Ki value is estimated to be 110 nM for S1P3 receptor.

DBCO-PEG4-MMAF is a drug-linker conjugate for ADC with potent antitumor activity by using the tubulin polymerization inhibitor, MMAF, linked via the cleavable linker DBCO-PEG4.

ACBI3 is a selective, potent and in vivo active pan-KRAS PROTAC degrader, potently degrades 13 out of 17 of the most prevalent oncogenic KRAS alleles (DC50=3.9 nM in GP2d cells).

Rocaglamide is a potent NF-κB activation inhibitor.

20-O-Acetylingenol-3-angelate is a natural compound.