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tolerability

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25

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-P99116
    Faricimab

    RG7716

    		 VEGFR Cardiovascular Disease Metabolic Disease Inflammation/Immunology
    Faricimab, an overall good safety and tolerability profile, is a bispecific antibody targeting Angiopoietin-2 (Ang-2) and vascular endothelial growth factor-A (VEGF-A). Faricimab prevents retinal vascular leakage, cell death and inflammation in retinal ischemia/reperfusion (I/R) injury and sCNV mouse models. Faricimab demonstrates statistically superior visual acuity gains versus Ranibizumab (HY-P9951). Faricimab can be used for retinal diseases, such as age-related macular degeneration (w-AMD), diabetic macular edema (DME) and macular edema following retinal vein occlusion (RVO) .
    Faricimab
  • HY-100656
    Desmethyl cariprazine

    		Dopamine Receptor 5-HT Receptor Drug Metabolite Neurological Disease
    Desmethyl cariprazine is an active metabolite of Cariprazine . Cariprazine, an antipsychotic agent candidate, exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (2.6 nM) .
    Desmethyl cariprazine
  • HY-143889
    Senexin C

    		CDK Cancer
    Senexin C is a selective and orally active CDK8/19 inhibitor. Senexin C shows a strong tumor-enrichment pharmacokinetic (PK) profile and tumor-pharmacodynamic (PD) marker responses. Senexin C inhibits the growth of MV4-11 leukemia cells with good tolerability .
    Senexin C
  • HY-17552
    sn-Glycero-3-phosphocholine
    1 Publications Verification

    Choline Alfoscerate; Alpha-GPC; L-α-GPC

    		 Cholinesterase (ChE) Endogenous Metabolite Neurological Disease
    sn-Glycero-3-phosphocholine (Choline Alfoscerate) is a precursor in the biosynthesis of brain phospholipids and increases the bioavailability of choline in nervous tissue. sn-Glycero-3-phosphocholine (Choline Alfoscerate) has significant effects on cognitive function with a good safety profile and tolerability, and is effective in the treatment of Alzheimer's disease and dementia .
    sn-Glycero-3-phosphocholine
  • HY-145294
    ROCK2-IN-5

    		ROCK Neurological Disease
    ROCK2-IN-5 (compound 1d) is a hybrid compound containing structural fragments of the Rho kinase inhibitor fasudil and the NRF2 inducers caffeic and ferulic acids. ROCK2-IN-5 has good multitarget profile and good tolerability. ROCK2-IN-5 has the potential for thr research of Amyotrophic lateral sclerosis (ALS) with a SOD1 mutation .
    ROCK2-IN-5
  • HY-132289
    Lipid M

    		Liposome Inflammation/Immunology
    Lipid M (pKa: 6.75) can be used to deliver mRNA vaccine and yield a robust immune response with improved tolerability .
    Lipid M
  • HY-14919
    Denibulin

    MN-029 free base

    		 Microtubule/Tubulin Cancer
    Denibulin, a novel vascular-disrupting agent, inhibits microtubule assembly reversibly, disrupting tumor vascular endothelial cell cytoskeletons. Denibulin demonstrated tolerability and potential anti-vascular effects, warranting further investigation in cancer therapy .
    Denibulin
  • HY-158012
    LY3056480

    		γ-secretase Others
    LY3056480 is a gamma-secretase inhibitor (GSI) that inhibits Notch signaling. LY3056480 improves mild to moderate sensorineural hearing loss and is safe and tolerable. Intratympanic administration of LY3056480 induces hair cell regeneration and partial hearing recovery in mammals .
    LY3056480
  • HY-161952
    JAB-3312

    		SHP2 Cancer
    JAB-3312 is an orally effective anticancer phosphatase SHP2 inhibitor (IC50: 1.9 nM) with anti-cancer activity. JAB-3312 has good tolerability and significantly induced tumor regression in a KYSE-520 mouse xenograft model .
    JAB-3312
  • HY-162572
    Bitipazone

    		Parasite Infection
    Bitipazone, diacetylbis(piperidinethyl)thiourea cysteine ??ester (I), has potent anticoccidial activity. Bitipazone showed significant efficacy and good tolerability in rabbits and turkeys, and in chronic toxicity tests, bitipazone was tolerated in turkeys at concentrations below 90 ppm in feed. Pharmacokinetic studies show that bitipazone is eliminated slowly from the blood and organs of these animal species .
    Bitipazone
  • HY-117259
    Valiltramiprosate

    ALZ-801

    		 Amyloid-β Neurological Disease
    ALZ-801 is a potent and orally available small-molecule β-amyloid (Aβ) anti-oligomer and aggregation inhibitor, valine-conjugated proagent of Tramiprosate with substantially improved PK properties and gastrointestinal tolerability compared with the parent compound . ALZ-801 is an advanced and markedly improved candidate for the treatment of alzheimer’s disease .
    Valiltramiprosate
  • HY-112090
    ABBV-744
    5 Publications Verification

    		 Epigenetic Reader Domain HIV Infection Inflammation/Immunology Cancer
    ABBV-744 is a first-in-class, orally active and selective inhibitor of the BDII domain of BET family proteins with IC50 values ranging from 4 to 18 nM for BRD2, BRD3, BRD4 and BRDT. ABBV-744 is primarily metabolized by CYP3A4 with agent-like properties enable the investigation of its antitumor efficacy and tolerability .
    ABBV-744
  • HY-144863
    BAY 1214784

    		GnRH Receptor Cancer
    BAY 1214784 is a potent, selective, and orally active antagonist of the human gonadotropin-releasing hormone receptor (hGnRH-R). BAY 1214784 is a spiroindoline derivative compound. BAY 1214784 effectively lowers plasma luteinizing hormone levels by up to 49%, at the same time being associated with low pharmacokinetic variability and good tolerability. BAY 1214784 has the potential for the research of uterine fibroids .
    BAY 1214784
  • HY-131364
    Nur77 modulator 1

    		Nuclear Hormone Receptor 4A/NR4A Apoptosis Cancer
    Nur77 modulator 1 is a good Nur77 binder (KD = 3.58 μM). Nur77 modulator 1 up-regulates Nur77 expression, mediates sub-cellular localization of Nur77, induces Nur77-dependent ER stress and autophagy, and results in cell apoptosis. Anti-hepatoma activity .
    Nur77 modulator 1
  • HY-156483
    TT-012

    		Others Cancer
    TT-012 specifically binds to dynamic MITF and destroys the latter's dimer formation and DNA-binding ability. TT-012 inhibits the transcriptional activity of MITF in B16F10 melanoma cells. TT-012 inhibits the growth of high-MITF melanoma cells, and inhibits the tumor growth and metastasis with tolerable toxicity to liver and immune cells in animal models .
    TT-012
  • HY-103019E
    Enitociclib

    BAY-1251152; VIP152

    		 Others Others
    Enitociclib (VIP152; BAY-1251152) is a selective CDK9 inhibitor. Known for its unique benzyl sulfoxide moiety, VIP152 has demonstrated promising efficacy and tolerability both in vitro and in vivo, including in mouse and rat xenograft models via weekly intravenous infusions Highly effective and well tolerated. VIP152 shows promising long-term single-agent inhibitory activity against double-click refractory diffuse large B-cell lymphoma .
    Enitociclib
  • HY-17552S
    sn-Glycero-3-phosphocholine-d9

    Choline Alfoscerate-d9; Alpha-GPC-d9; L-α-GPC-d9

    		 Isotope-Labeled Compounds Cholinesterase (ChE) Endogenous Metabolite Neurological Disease
    sn-Glycero-3-phosphocholine-d9 is the deuterium labeled sn-Glycero-3-phosphocholine. sn-Glycero-3-phosphocholine (Choline Alfoscerate) is a precursor in the biosynthesis of brain phospholipids and increases the bioavailability of choline in nervous tissue. sn-Glycero-3-phosphocholine (Choline Alfoscerate) has significant effects on cognitive function with a good safety profile and tolerability, and is effective in the treatment of Alzheimer's disease and dementia[1][2].
    sn-Glycero-3-phosphocholine-d9
  • HY-10063
    Ispronicline

    TC-1734; ACD3480

    		 nAChR Neurological Disease
    Ispronicline (TC-1734), an orally active, brain-selective α4β2 nicotine acetylcholine receptor (nAChR) partial agonist, has shown memory-enhancing properties in rodents and a good tolerability profile. Ispronicline binds to the α4β2 nAChR with high affinity (Ki=11 nM) and is highly selective to other nAChRs such as α7 nAChR and α3β4 nAChR .
    Ispronicline
  • HY-14913
    Apricitabine

    SPD754; AVX754

    		 Nucleoside Antimetabolite/Analog HIV DNA/RNA Synthesis Infection
    Apricitabine (SPD754; AVX754), the (-) enantiomer of 2′-deoxy-3′-oxa-4′-thiocytidine (dOTC), is a highly selective and orally active HIV-1 reverse transcriptase (RT) inhibitor (Ki=0.08 μM), as well as inhibits DNA polymerases α, β, and γ with Ki value of 300 μM, 12 μM, and 112.25 μM, respectively . Apricitabine (SPD754; AVX754) shows promising antiretroviral efficacy, good tolerability and a low propensity for resistance selection in antiretroviral-naive HIV infection [2].
    Apricitabine
  • HY-162720
    NNRT-IN-4

    		HIV Potassium Channel Reverse Transcriptase Infection
    NNRT-IN-4 (Compound 10p) is an inhibitor for non-nucleoside reverse transcriptase (NNRT) with an IC50 of 0.713 µM for HIV-1 RT. NNRT-IN-4 exhibits antiviral efficacy, inhibits HIV-1 wildtype and mutant strains with EC50 of 6-63 nM. NNRT-IN-4 exhibits a slight inhibitory activities against hERG (IC50=25.9 µM) and CYP enzymes (IC50>50 µM). NNRT-IN-4 exhibits good tolerability and safety in mice (2 g/kg) .
    NNRT-IN-4
  • HY-P99974
    Nab-Paclitaxel

    Nanoparticle albumin-bound Paclitaxel; Nanoparticle albumin-bound ABI-007

    		 Microtubule/Tubulin Apoptosis Autophagy Cancer
    Nab-Paclitaxel is an albumin-bound nanoparticle formulation of Paclitaxel (HY-B0015). Nab-Paclitaxel is composed of albumin and the active pharmaceutical ingredient Paclitaxel (Paclitaxel: human albumin=1:9), in which human albumin is used as an excipient to disperse and stabilize particles and carry the main drug. Nab-Paclitaxel was associated with higher response rates and better tolerability, with favorable pharmacokinetic properties . (The product size below only indicate the effective content of Paclitaxel. The actual albumin quality depends on the batch. The ratio of each component in this product is Paclitaxel: albumin = 1:7-1:11.)
    Nab-Paclitaxel
  • HY-156498
    RMC-7977

    		Ras ERK Raf Ribosomal S6 Kinase (RSK) AMPK Apoptosis PARP Cancer
    RMC-7977 is an orally active triple-complex RAS inhibitor that can simultaneously bind to cyclophilin A (CYPA) (Kd = 195 nM) and KRAS (G12V) (Kd = 292 μM). It exhibits broad-spectrum inhibitory activity against KRAS, NRAS, and HRAS proteins and their various wild-type and mutant variants. RMC-7977 induces apoptosis by inhibiting the phosphorylation of ERK, CRAF, and RSK, as well as increasing PARP cleavage. This leads to tumor regression, reduces resistance in KRAS G12C cancer models, and demonstrates good tolerability across various RAS cancer models .
    RMC-7977
  • HY-P3375
    Mazdutide

    IBI-362; LY-3305677; OXM-3

    		 GCGR GLP Receptor Metabolic Disease
    Mazdutide (IBI-362; LY-3305677) is a long-acting synthetic oxyntomodulin analog. Mazdutide is also a co-agonist of glucagon-like peptide (GLP-1R) and glucagon receptor (GCGR). Mazdutide binds human and mouse GCGR (Ki: 17.7 nM and 15.9 nM, respectively) and GLP-1R (Ki: 28.6 nM and 25.1 nM, respectively) and stimulates insulin secretion from mouse islets (EC50: 5.2 nM). Mazdutide is used in studies of obesity and type 2 diabetes (T2D) .
    Mazdutide
  • HY-P3375A
    Mazdutide TFA

    IBI-362 TFA; LY-3305677 TFA; OXM-3 TFA

    		 GCGR GLP Receptor Metabolic Disease
    Mazdutide (IBI-362; LY-3305677) TFA is a long-acting synthetic oxyntomodulin analog. Mazdutide is also a co-agonist of glucagon-like peptide (GLP-1R) and glucagon receptor (GCGR). Mazdutide TFA binds human and mouse GCGR (Ki: 17.7 nM and 15.9 nM, respectively) and GLP-1R (Ki: 28.6 nM and 25.1 nM, respectively) and stimulates insulin secretion from mouse islets (EC50: 5.2 nM). Mazdutide TFA is used in studies of obesity and type 2 diabetes (T2D) .
    Mazdutide TFA
  • HY-117947
    (R)-OR-S1

    		Others Cancer
    (R)-OR-S1 is an isomer of OR-S1. The dual ZH1/2 inhibitors OR-S1 and OR-S2 exhibit strong inhibitory activity against both EZH1 and EZH2. OR-S1 and OR-S2 are highly selective methyltransferase inhibitors against EZH1 and EZH2, and they have very similar molecular features. Therefore, we investigated the effect of OR-S1 on acute myeloid leukemia (AML). We found that OR-S1 was able to induce cell differentiation and apoptosis in AML cells. These findings encouraged us to investigate whether functional LT-HSCs could survive PRC2-targeted therapy with OR-S1 or OR-S1 combined with cytarabine. The results showed that OR-S1 did not cause significant myelosuppression, and BM cells treated with the combination therapy were able to undergo normal hematopoiesis even 4 months after treatment. Therefore, temporary inhibition of EZH1 and EZH2 is clinically tolerable, making this combination therapy suitable for AML patients. AML is generally believed to originate from myeloid progenitor cells that inherit a large number of biological properties.
    (R)-OR-S1

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