Tanurubat (ANX005) (at titration concentration) has a high and comparable affinity for C1q derived from human, cynomolgus monkey, rhesus monkey, dog and rat serum, a low affinity for mouse C1q, and does not bind to rabbit C1q [1]. Tanurubat (at titration concentration; 1 hour) effectively inhibits classical complement-mediated hemolysis in human, cynomolgus monkey, rhesus monkey, dog and rat serum with an average IC50 of approximately 350 ng/mL, but does not inhibit hemolysis in rabbit serum [1].

Tanruprubart (ANX005) (10-200 mg/kg; intravenous injection; once a week; 4 weeks) was administered to Sprague Dawley rats for 4 consecutive weeks, resulting in dose-dependent exposure of serum and cerebrospinal fluid, complete depletion of measurable levels of free serum C1q, and no treatment-related toxicity was observed at doses up to 200 mg/kg, resulting in a no-observed adverse event level (NOAEL) of 200 mg/kg [1]. Tanruprubart (ANX005) (10–200 mg/kg; intravenous injection; single bolus injection; once weekly for 4 weeks) produced dose-dependent serum and cerebrospinal fluid exposure, completely depleted free serum C1q, and inhibited complement-mediated hemolysis at measurable reagent levels, completely occupied cerebrospinal fluid C1q at high doses, and showed no treatment-related toxicity at doses up to 200 mg/kg, resulting in a No Observed Adverse Effect Level (NOAEL) of 100 mg/kg[1].

Animal/Disease Models:Sprague Dawley rats (male and female, young adults, 8-9 weeks old)[1]
Doses: 10 mg/kg; 50 mg/kg; 100 mg/kg; 200 mg/kg
Route of Administration: Intravenous injection; once a week for 4 weeks
Experimental Results: Reduced the concentration of free C1q in rat serum to measurable reagent levels. Serum Cmax increased in a dose-proportional manner; in the lower dose range, the increase in AUC was greater than the dose-proportional; while in the dose range of 100 to 200 mg/kg, the increase in AUC was proportional to the dose-proportional. The mean cerebrospinal fluid concentration increased in a greater-than-dose-proportional manner, and on days 38 and 50 of the GLP study, the cerebrospinal fluid concentration was 0.1% to 0.2% of the serum concentration. No treatment-related changes in clinical symptoms, weight, food consumption, clinicopathology, gross pathology, organ weight, or histopathology were observed at any of the tested doses. The No Observed Adverse Effect Level (NOAEL) was 200 mg/kg.

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Animal/Disease Models:Crab-eating macaques (male and female, 2-4 years old)[1]
Doses: 15 mg/kg (single bolus); 100 mg/kg (single bolus); 10 mg/kg (once a week for 4 weeks); 50 mg/kg (once a week for 4 weeks); 100 mg/kg (once a week for 4 weeks); 200 mg/kg (once a week for 4 weeks)
Route of Administration: Intravenous injection; single bolus; once a week; 4 weeks
Experimental Results: At measurable reagent concentrations, free C1q in monkey serum was completely eliminated, and only when the reagent concentration was reduced below the detection limit did free C1q return to baseline levels. At measurable reagent serum concentrations, in vitro complement-mediated hemolysis was completely inhibited, and hemolytic activity returned to baseline levels as the reagent concentration decreased. Serum concentrations increased in a dose-dependent manner, with trough concentrations gradually accumulating after weekly dosing in the 50, 100, and 200 mg/kg groups (excluding animals exhibiting anti-antibody responses). Mean cerebrospinal fluid (CSF) concentrations increased with increasing dose; in non-GLP studies, CSF concentrations ranged from 0.04% to 0.11% of serum concentrations, while in GLP studies, CSF concentrations ranged from 0.02% to 0.13% of serum concentrations on day 29. On day 29, at 100 and 200 mg/kg doses, C1q was completely occupied in the CSF. No treatment-related changes were observed in clinical symptoms, body weight, food consumption, clinicopathology, gross pathology, organ weight, histopathology, ophthalmological findings, neurological examination, vital signs, or electrocardiogram at any tested dose. The No Observed Adverse Effect Level (NOAEL) was 200 mg/kg.

[1]. Nonclinical Development of ANX005: A Humanized Anti-C1q Antibody for Treatment of Autoimmune and Neurodegenerative Diseases. Int J Toxicol. 2017;36(6):449-462.

PLEASEREFERTOTHELOT-SPECIFICCOAFORSPECIFICBUFFERINFORMA

145.78 kDa

2065212-40-8

Cell-ATP Viability Detection Kit; Protein A Agarose; HOLO Human Interleukin-2 (IL-2) Detection Kit; Bradford Protein Assay Kit; Cell Counting Kit-8

Colorless to light yellow liquid

ANX005

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)