| DC49622 |
A-61603
Featured
|
A-61603 is a selective α1A-adrenergic receptor agonist. A-61603 increases the frequency of spontaneous Ca2+ transients in rat ventricular myocytes in vitro. |
|
| DC49647 |
MNI137
Featured
|
MNI137 is a potent and selective negative allosteric modulator for group II mGluRs. MNI137 has IC50s values of 8.3 and 12.6 nM for human and rat mGlu2 inhibition of glutamate-induced calcium mobilization. |
|
| DC49650 |
Y1R probe-1
Featured
|
Y1R probe-1 (Compound 39) is a high-affinity fluorescence probe for the Neuropeptide Y Y1 Receptor. Y1R probe-1 has the potential for the research of cancer disease. |
|
| DC49661 |
AGI-43192
Featured
|
AGI-43192 is a potent inhibitor of methionine adenosyltransferase 2A (MAT2A). AGI-43192 is a potent, but limited brain-penetrant compound. AGI-43192 has the potential for exploring the effects of SAM modulation in the central nervous system (CNS) and research of cancer disease. |
|
| DC49664 |
H2L5186303
Featured
|
H2L5186303 is a potent and selective LPA2 receptor (lysophosphatidic acid 2 receptor) antagonist with an IC50 of 9 nM. |
|
| DC49673 |
STING agonist-7
Featured
|
STING agonist-7 is a non-nucleotide STING agonist. STING agonist-7 binds selectively to mouse STING but not human STING. STING agonist-7 penetrates cell membrane poorly. |
|
| DC49675 |
D18
Featured
|
D18 is an immune modulator. D18 acts as a TLR7/8 dual agonist (EC50=24 nM for hTLR7 and 10 nM for hTLR8, respectively). D18 increases PD-L1 expression through epigenetic regulation, thus sensitizing tumors to PD-1/PD-L1 blockade. D18 is a ADC cytotoxin uesd for the systhesis of ADC HE-S2. |
|
| DC49692 |
T-Type calcium channel inhibitor(TTA-P2)
Featured
|
T-Type calcium channel inhibitor is a potent inhibitor of T-Type calcium channel. T-Type calcium channel inhibitor penetrates well the CNS and blocks the native T-type currents in deep cerebellar nuclear neurons, the window current is completely abolished both for wild-type and mutant Cav3.1 channels. T-Type calcium channel inhibitor has the potential for the research of neurology disease. |
|
| DC49710 |
KM91104
Featured
|
KM91104, a cell-permeable V-ATPase inhibitor, specifically targets the a3-b2 subunits of V-ATPase. |
|
| A724 |
Girentuximab
Featured
|
Girentuximab (G250) is a chimeric monoclonal antibody that binds carbonic anhydrase IX (CAIX), a cell surface glycoprotein ubiquitously expressed in clear cell renal cell carcinoma (ccRCC). |
|
| DC49760 |
THP104c
Featured
|
THP104c is a mitochondrial fission inhibitor. |
|
| DC49761 |
BAY-179
Featured
|
BAY-179 is a potent, selective, and species cross-reactive complex I inhibitor (IC50=79 µM). |
|
| A126 |
Evolocumab Biosimilar （Anti-PCSK9 Reference Antibody）
Featured
|
Evolocumab (AMG 145) is a human monoclonal antibody that inhibits PCSK9. Evolocumab binds to the circulating PCSK9 protein, inhibiting it from binding to the LDLR. Evolocumab can be used for the research of hypercholesterolemia and atherosclerotic cardiovascular diseases. |
|
| DC49826 |
AZD-9574
Featured
|
AZD9574 is a CNS-penetrant, PARP1-selective inhibitor with IC50 of <0.005 μM. AZD9574 demonstrates >10,000-fold selectivity for PARP1 over PARP2 and shows excellent preclinical PK acrossseveral species, with low clearance and high oral bioavailability, and demonstrated in vivo efficacy in a BRCA2−/− DLD-1 mouse xenograft model. |
|
| DC49844 |
ELOVL1-IN-2
Featured
|
ELOVL1-IN-2 is an elongation of very long chain fatty acid 1 (ELOVL1) enzyme inhibitor, ELOVL1-IN-2 shows weak ELOVL1 inhibition (IC50=21 μM) and moderate potency in a primary cellular assay (HEK293 C26 IC50=6.7 μM) . |
|
| DC49845 |
TT3
Featured
|
TT3 is an ionizable cationic amino lipid that has been used in combination with other lipids in the formation of lipid-like nanoparticles (LLNs). Administration of LLNs containing TT3 and encapsulating mRNA encoding human coagulation Factor IX induces human coagulation Factor IX expression in the plasma of mice. |
|
| DC49858 |
Dodecyltrimethylammonium bromide
Featured
|
Dodecyltrimethylammonium bromide (DTAB) is a surfactant. Dodecyltrimethylammonium bromide interacts with DNA and changes the mechanical properties of DNA on binding and the specific binding parameters of the interaction. |
|
| DC49861 |
Pseudouridine 5'-triphosphate
Featured
|
pseudouridine-5’-triphosphate (Pseudo-UTP) is one of the most commonly used modified nucleoside for the polymerase-mediated synthesis of RNA molecules. Compared with uridine-containing unmodified mRNAs, the application of pseudouridine-containing modified mRNAs exhibits better nuclease stability, immunogenicity, and translational properties. |
|
| DC49871 |
hGPR91 antagonist 3
Featured
|
hGPR91 antagonist 3 (Compound 5g) is a potent, selective, and orally active antagonist of hGPR91 (%F: 26). hGPR91 antagonist 3 has the potential for the research of hypertension, autoimmune disease and retinal angiogenesis. |
|
| DC49872 |
GSK854
Featured
|
GSK854 is a potent Inhibitor of Troponin I-Interacting Kinase (TNNI3K). GSK854 is a suitable lead for identifying new cardiac medicines and have been employed as in vivo tools in investigational studies aimed at defining the role of TNNI3K within heart failure. |
|
| DC49882 |
CKK-E12
Featured
|
CKK-E12 is a ionizable lipid in combination with other lipids make up the lipid nanoparticles which are used to deliver RNA-based therapeutics. cKK-E12 was highly selective toward liver parenchymal cell in vivo.Multitail lipids usually have three or more tails and tend to form
more cone-shaped structures due to the increase of tail crosssection,
which enhances the endosome escape and mRNA
delivery efficiency.CKK-E12 is an ionizable lipid with four
lipid tails and diketopiperazine core-based head. It has shown
excellent efficiency in delivering CRISPR-Cas9 mRNA and
sgRNA.cKK-E12 iLNPs encapsulated mRNA was used to
investigate the effect of Toll-like receptor 4 (TLR4) on iLNPsmediated
mRNA delivery, and it has been demonstrated that
the targeting, safety and efficacy of iLNPs are closely related
to disease state. In other words, even though iLNP delivers
therapeutic mRNA to a given cell type in one disease state, it
is not guaranteed to deliver mRNA to the same cell type in
another disease. As same as MC3 and C12-200, CKK-E12 is also
used to be a positive control ionizable lipid when exploiting new
ionizable lipids. |
|
| DC49883 |
L343
Featured
|
L-343 is an ionizable cationic lipidoid and can be used to synthetic liposomes for systemic delivery of RNAi therapeutics, Pka: 6.34.L343, with its sterically hindered tert-butyl esters, exhibited slower elimination from plasma and higher and more persistent levels in liver compared with L319. |
|
| DC49889 |
503O13
Featured
|
503O13 is a next-generation, biodegradable lipid nanoparticle (LNP) engineered for highly efficient and targeted siRNA delivery. Designed through rational structure-activity criteria—including optimal tail length (O13), tertiary amines, and a surface pKa ≥5.5—this single-component LNP achieves unparalleled gene silencing with an ultra-low EC50 of 0.01 mg/kg in preclinical models.503O13 outperforms non-degradable counterparts (e.g., C12-200) with improved toxicity profiles—no hepatic necrosis or pancreatic inflammation—while maintaining rapid blood clearance (t1/2: 6 min) and organ-specific accumulation (liver/spleen). |
|
| A127 |
Rovalpituzumab Biosimilar （Anti-DLL3 Reference Antibody）
Featured
|
Rovalpituzumab is a humanized monoclonal antibody against delta-like protein 3 (DLL3). Rovalpituzumab can be used in the synthesis of antibody-drug conjugate (ADC), Rovalpituzumab Tesirine. Rovalpituzumab has activity against small cell lung cancer (SCLC). |
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|
| DC49907 |
5A2-SC8
Featured
|
5A2-SC8 is a dendrimer for miRNA delivery to late-stage liver tumors with low hepatotoxicity. 5A2-SC8 shows potent EC50 < 0.02 mg/kg (siRNA against FVII (siFVII)) in dose-response experiments, and well tolerated in separate toxicity studies in chronically ill mice bearing MYC-driven tumors. 5A2-SC8 is a degradable lipid-like compound (ester-based dendrimer) for small RNAs delivery.5A2-SC8, was obtained by screening a large library of more than 1500 ester-based dendrimers
containing ionizable amino groups, which have three
tertiary amine heads and five lipid tails. Based on this library,
the in vitro transfection efficiency of different formulations of
5A2-SC8 iLNPs was evaluated, discovering the optimal formulation
(5A2-SC8, DOPE, cholesterol, PEG at a molar ratio of
15:15:30:3) of 5A2-SC8 iLNPs for delivering fumarylacetoacetate
hydrolase (FAH) mRNA to liver.After the intravenous injection
via tail, the model mice of hepatorenal tyrosinemia type I
had strong FAH protein expression, which prevented
body weight loss and increased the survival rate of hepatorenal
tyrosinemia mice . In addition to introducing utility of
5A2-SC8 iLNPs for the therapeutic intervention, the 5A2-SC8
iLNPs containing DOTAP have been used to establish complex
mouse models via intravenous injection, including in situ liverspecific
cancer model and in situ lung-specific cancer model.
Based on this iLNPs delivery system, 5A2-SC8 induced model
construction method overcomes the time-consuming and costly
disadvantages of traditional animal models establishing methods,
including transgenesis and gene engineering in embryonic
stem cells. |
|
| DC49908 |
OF-02
Featured
|
OF-02 (OF-2) is an alkenyl amino alcohol (AAA) ionizable lipid for highly potent in vivo mRNA delivery.Alkenyl amino alcohols (AAA) are a functional group found in sphingosine and other bioactive molecules. It was used to prepare
AAA-based ionizable lipids through ring-opening reactions between alkenyl epoxides (AEs) and polyamine cores. These
AAA-based iLNPs could promote high-level protein expression Therefore, AAA-based ionizable lipids OF-00, OF-01,
OF-02, and OF-03 were prepared. The results of in vivo delivery
of human erythropoietin (hEPO) mRNA showed that the AAA
ionizable lipid OF-02 with the linoleic acid derivative
could effectively deliver hEPO mRNA. Compared with the positive
control CKK-E12, OF-02 showed an increased ability to
induce serum EPO protein expression by nearly twofold
(Figure 7b). Likewise, it outperformed two benchmark ionizable
lipids (503013 and C12-200) in the nucleic acid delivery field.
Furthermore, the mRNA delivered by OF-02 iLNPs was mainly
in vivo.translated into the liver. The liver-targeting ability of OF-02 iLNPs
improves their delivery efficiency. Therefore, the OF-02 iLNPs
may become excellent delivery vehicles for the treatment of liver
diseases without other side effects of damage to other organs
during the treatment |
|
| DC49915 |
DSPG-Na
Featured
|
DSPG-Na is the component of liposomes for drug delivery. |
|
| DC49919 |
FEN1-IN-SC13
Featured
|
FEN1-IN-SC13 is a potent DNA fragmentation endonuclease 1 (FEN1) inhibitor (CN106692155A, SC13). |
|
| DC49931 |
NVP-DKY709
Featured
|
NVP-DKY709 is a potent IKZF2 inhibitor for the treatment of cancers. |
|
| DC49932 |
FTT5
Featured
|
FTT5 is a lipid-like compound for efficient delivery of long mRNAs in vivo. |
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